Search Result
Results for "
inhibitory activities
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
16
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-N4142
-
Ideain chloride
|
Cholinesterase (ChE)
|
Cardiovascular Disease
|
Cyanidin-3-O-galactoside chloride (Ideain chloride) is a component from extract peel of hawthorn fruit (EPHF) with the value of 179.4 mg/g. EPHF exhibits strong AChE inhibitory activity .
|
-
-
- HY-N8671
-
|
Others
|
Neurological Disease
|
Withanoside V, a withanolide glycoside, exhibits inhibitory activity for tachyphylaxis to Clonidine in isolated guinea-pig ileum .
|
-
-
- HY-156031
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
BChE-IN-19 (Compound 7b) is a para-substituted derivative of indone (7b) with inhibitory activity of butyryl cholinesterase (BChE) (IC50=0.04 μM). BChE-IN-19 improves cholinergic scheduling in the nervous system. BChE-IN-19 can be used against Alzheimer's disease .
|
-
-
- HY-N11945
-
Kadsulignan J
|
NO Synthase
|
Others
|
Schiarisanrin A (Kadsulignan J) is a lignan with inhibitory activity on NO production. Schiarisanrin A inhibits NO production in BV-2 cells with an IC50 of 9.6 μM .
|
-
-
- HY-N11943
-
|
NO Synthase
|
Others
|
Kadsulignan H (compound 13) is a lignan with inhibitory activity on NO production. Kadsulignan H inhibits NO production in BV-2 cells with an IC50 of 14.1 μM .
|
-
-
- HY-N8604
-
|
Others
|
Inflammation/Immunology
|
Methyl 4-O-caffeoylquinate is an extract naturally
derived from the leaf ofIlex paraguariensis. Methyl
4-O-caffeoylquinate has human neutrophilic elastase (HNE) inhibitory activity
.
|
-
-
- HY-149018
-
|
Phosphodiesterase (PDE)
|
Cancer
|
ATX inhibitor 22 is a novel inhibitor of ATX (autotaxin) with IC50 of 218 nM but lost its inhibitory activity of LPAR1 .
|
-
-
- HY-151604
-
|
Transketolase
|
Others
|
Transketolase-IN-3 is a potent transketolase (TK) inhibitor. Transketolase-IN-3 has herbicidal activity and has inhibitory effects against Digitaria sanguinalis (DS) and Amaranthus retroflexus (AR). Transketolase-IN-3 can be used for the research of herbicides .
|
-
-
- HY-122963
-
|
Adenosine Receptor
|
Metabolic Disease
|
Danshenol B is a diterpenoid. Danshenol B has strong aldose reductase (AR) inhibitory activity with IC50 value of 0.042μM. Danshenol B can be used for the research of diabetic related complication resulted by metabolic abnormality, such as cataracts, retinopathy, neuropathy, and nephropathy .
|
-
-
- HY-131999
-
|
Others
|
Metabolic Disease
|
3,4,5-Trihydroxycinnamic acid decyl ester is an excellent inhibitor of lipid absorption and accumulation, with anti-obesity properties. 3,4,5-Trihydroxycinnamic acid decyl ester is a pancreatic lipase inhibitor, with an EC50 of approximately 0.9 μM .
|
-
-
- HY-146038
-
|
Apoptosis
ROS Kinase
MDM-2/p53
Bcl-2 Family
|
Cancer
|
Antitumor agent-55 (compound 5q) is a potent antitumor agent. Antitumor agent-55 effectively inhibits PC3, with an IC50 of 0.91 μM. Antitumor agent-55 effectively inhibits the colony formation, suppresses the cell migration in PC3. Antitumor agent-55 induces G1/S phase arrest and apoptosis in PC3 .
|
-
-
- HY-W017401
-
BIT
|
Others
|
Infection
|
Benzisothiazolone is an isothiazolone fungicide. Benzisothiazolone has growth inhibiting activity against E. coli ATCC 8739 and saccharornyces pombe NCYC 1354. Benzisothiazolone can be used in the study of growth inhibition model .
|
-
-
- HY-N8764
-
-
-
- HY-145112
-
-
-
- HY-156359
-
|
Others
|
Others
|
Tuberculosis inhibitor 10 shows moderate inhibitory effect on the enzymatic activity of MSMEG_6649. Tuberculosis inhibitor 10 enhances the inhibitory activity of PAS against mycobacteria .
|
-
-
- HY-120692
-
-
-
- HY-142100
-
|
NF-κB
|
Inflammation/Immunology
|
Licoagrochalcone C, a flavonoid, reveals efficacious inhibitory activity on NF-κB transcription. Licoagrochalcone C shows significant inhibitory activity on LPS (HY-D1056)-induced NO production .
|
-
-
- HY-N7717
-
(–)-(1R)-N-methylcoclaurine
|
Others
|
Metabolic Disease
|
(-)-N-methylcoclaurine possesses melanogenesis inhibitory activity .
|
-
-
- HY-139647
-
-
-
- HY-W027340
-
ARM1
1 Publications Verification
4BSA
|
Aminopeptidase
Epoxide Hydrolase
|
Cancer
|
ARM1 (4BSA) is a potent aminopeptidase and epoxide hydrolase inhibitor. ARM1 shows aminopeptidase inhibitory activity with an IC50 7.61 µM and epoxide hydrolase inhibitory activity with an IC50 12.4 µM .
|
-
-
- HY-N9330
-
-
-
- HY-N2461
-
-
-
- HY-P2157
-
|
Ras
|
Cancer
|
Ras Inhibitory Peptide (VPPPVPPRRR) is a Ras inhibitor with antitumor activity .
|
-
-
- HY-P3578
-
|
Insulin Receptor
|
Endocrinology
|
Gastric Inhibitory Polypeptide (1-30), porcine lacks the C-terminal 12 amino acid residues of natural gastric inhibitory polypeptide (GIP), exhibits biologic activity by potentiating the release of insulin and somatostatin .
|
-
-
- HY-114437
-
Z-D-Phe-Phe-Gly-OH; FIP; Virus Replication inhibitory Peptide
|
Influenza Virus
|
Infection
|
Fusion Inhibitory Peptide (Z-D-Phe-Phe-Gly-OH, FIP, Virus Replication Inhibitory Peptide) is a potent inhibitor of the virus replication, by inhibiting the membrane fusing activity of a viral glycoprotein .
|
-
-
- HY-122790
-
|
Bacterial
|
Infection
|
2-Hydroxydocosanoic acid has antioxidant, cholinesterase inhibitory, and antimicrobial activities .
|
-
-
- HY-143884
-
|
JAK
|
Inflammation/Immunology
|
JAK2/TYK2-IN-2 is a potent and selective TYK2 inhibitor with IC50 values of 9 and 157 nM for TYK2 and JAK2, respectively. JAK2/TYK2-IN-2 has anti-inflammatory activity .
|
-
-
- HY-144190
-
-
-
- HY-W278232
-
|
Bacterial
|
Infection
|
Urease-IN-6 is a potent inhibitor of Urease with an IC50 of 14.2 μM. Urease-IN-6 can be used in study peptic and gastric ulcers .
|
-
-
- HY-N2898
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
Artanin is a coumarin, has biological activities related to Alzheimer’s disease. Artanin exerts function including AChE inhibitory and AChE- and self-induced amyloid beta (Aβ) aggregation inhibitory activities, with IC50s of 51 μM, 98 μM, and 124 μM, respectively .
|
-
-
- HY-101577
-
-
-
- HY-N7996
-
|
Bacterial
Fungal
|
Infection
|
Matairesinoside is a lignan with antibacterial and antioxidant activities. Matairesinoside also shows virus-cell fusion inhibitory activity .
|
-
-
- HY-U00332
-
6,6'-Oxybis[2,2-dimethyl-1-hexanol]
|
Others
|
Metabolic Disease
|
Hydrocarbon chain derivative 1 is an active compound, with inhibitory activities against lipid synthesis.
|
-
-
- HY-101404
-
|
Endogenous Metabolite
|
Others
|
DL-Homocysteine thiolactone hydrochloride is a cyclic amino acid derivative that exhibits root-growth inhibitory activity.
|
-
-
- HY-141874
-
-
-
- HY-119596
-
|
Xanthine Oxidase
|
Others
|
Eupatoriochromene is a chromene and has inhibitory activity against xanthine oxidase (XO) .
|
-
-
- HY-N12370
-
|
Others
|
Others
|
Tenaxin I is a component extracted from Radix Scutellariae with neuraminidase inhibitory activity .
|
-
-
- HY-139857
-
|
Tyrosinase
|
Others
|
Piceid 6″-O-azelaic acid ester shows high intracellular tyrosinase inhibitory and depigmentating activities.
|
-
-
- HY-145115
-
|
Others
|
Infection
|
Adeninobananin, a negative control tool, does not show any inhibitory activity of the SARS Coronavirus helicase.
|
-
-
- HY-N10286
-
|
Tyrosinase
|
Others
|
Chetoseminudin B possesses mushroom tyrosinase inhibitory activity with IC50 of 31.7 μM .
|
-
-
- HY-137220
-
-
-
- HY-N0539
-
|
Aldose Reductase
|
Cancer
|
Calceolarioside B is a natural product isolated from Akebia quinata leaves. Calceolarioside B exhibits significant inhibitory activity against rat lens aldose reductase (RLAR) with an IC50 of 23.99 μM. Calceolarioside B displays inhibitory effect on DPPH radical scavenging activity with an IC50 of 94.60 μM .
|
-
-
- HY-119804
-
|
Cytochrome P450
|
Neurological Disease
|
Licopyranocoumarin is an isoflavonoid that shows CYP3A4 inhibitory activity with an IC50 of 32 μM. Licopyranocoumarin has potent neuroprotective activities .
|
-
-
- HY-N7128
-
|
Cytochrome P450
|
Cancer
|
Flavanone is a naturally occurring flavone. Flavanone has inhibitory activity for human estrogen synthetase (aromatase) .
|
-
-
- HY-N2465
-
|
Others
|
Inflammation/Immunology
|
Methylsticin is a kavalactone isolated from the Piper methysticum . Methylsticin exhibit osteoclast formation inhibitory activity .
|
-
-
- HY-122308
-
|
Others
|
Metabolic Disease
|
Militarine, a glycosidic compound isolated from Bletilla striata, exhibits plant growth-inhibitory activity .
|
-
-
- HY-N7929
-
|
Tyrosinase
|
Cancer
|
5-Feruloylquinic acid (5-FQA) possesses antioxidative effects and tyrosinase inhibitory activities .
|
-
-
- HY-133804
-
|
Others
|
Metabolic Disease
|
Arteanoflavone, a natural compound that can be isolated from A. iwayomogi, possess inhibitory activities on AGEs formation .
|
-
-
- HY-N2827
-
(-)-Aglain C
|
Others
|
Others
|
Aglain C is isolated from A. ponapensis. Aglain C enhances the NF-kB inhibitory activity .
|
-
-
- HY-160657
-
|
Others
|
Others
|
DC-TEADin04 has weak inhibitory activity against TEAD4 palmitoylation .
|
-
- HY-147730
-
|
HDAC
|
Cancer
|
A variety of compounds were designed and synthesized by modifying cap groups. The enzyme inhibition test showed that compound 12C had broad-spectrum enzyme inhibitory activity, and compounds 9m and 9q were more inclined to inhibit HDAC6, showing a certain selective inhibitory activity among the representative subtypes.
|
-
- HY-N7993
-
-
- HY-16698
-
|
Others
|
Cancer
|
kb-NB77-78 is an analogue of CID797718, but shows no PKD inhibitory activity .
|
-
- HY-N2176
-
(+)-Marmesin; (S)-Marmesin
|
COX
Lipoxygenase
|
Others
|
S-(+)-Marmesin is a natural coumarin, exhibiting COX-2/5-LOX dual inhibitory activity.
|
-
- HY-N6055
-
|
Influenza Virus
|
Infection
|
Nuezhenidic acid can be isolated from the fruits of Ligustrum lucidum, posseses inhibitory activities against influenza A virus .
|
-
- HY-125437
-
-
- HY-143206
-
|
Elastase
|
Others
|
Tyrosinase/elastase-IN-1 a triterpenoid from Rubus fraxinifolius leaves, has tyrosinase and elastase inhibitory activities.
|
-
- HY-101087
-
|
Carbonic Anhydrase
|
Cancer
|
Benzenesulphonamide (compound 1) is a potent carbonic anhydrase inhibitor. Benzenesulphonamide shows CA II inhibitory activity .
|
-
- HY-N9834
-
-
- HY-151502
-
-
- HY-N10871
-
|
Others
|
Cancer
|
Neocryptomerin, a biflavonoid, shows inhibitory activity against U251, MCF-7, HeLa cell .
|
-
- HY-121106
-
|
Others
|
Others
|
9-Deazaguanine is a nucleoside analog with potent inhibitory activity against purine nucleoside phosphorylase (PNP) .
|
-
- HY-123550
-
-
- HY-156051
-
|
HCV
|
Infection
|
Tetrazolast is a HCV inhibitor with the inhibitory activity ranging from 5% to 20%, extracted from patent WO2005030774.
|
-
- HY-N3392
-
-
- HY-N8427
-
-
- HY-161289
-
|
Tyrosinase
|
Cancer
|
Tyrosinase-IN-24 (compound 3b) is a tyrosinase inhibitor with inhibitory activity against mushroom tyrosinase .
|
-
- HY-143900
-
|
Btk
Apoptosis
|
Inflammation/Immunology
Cancer
|
BTK-IN-7 is a potent and selective inhibitor of BTK (IC50=4.0 nM). BTK-IN-7 has high selectivity in both enzymatic (ITK >250-fold, EGFR >2500-fold) and cellular levels (ITK >227-fold, EGFR 27-fold). BTK-IN-7 also has potent antitumor activity .
|
-
- HY-124782
-
|
HDAC
|
Infection
|
HDAC8-IN-8 (15a) is an HDAC8 inhibitor, with IC50 values of 23.9 μM and 268.2 μM for hHDAC8 and smHDAC8 respectively. And for hHDAC1 and hHDAC6, the IC50 values are 12.1 μM and 2.9 μM respectively. HDAC8-IN-8 can be used in schistosomiasis-related research .
|
-
- HY-P4810
-
T140
|
CXCR
|
Infection
|
Polyphemusin II-Derived Peptide (T140), a CXCR4 inhibitor, shows high inhibitory activity against HIV-1 entry and the inhibitory effect on the binding of an anti-CXCR4 monoclonal antibody (12G5) to CXCR4 .
|
-
- HY-133146
-
|
Phosphatase
Apoptosis
|
Inflammation/Immunology
|
DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration .
|
-
- HY-77195
-
|
Polo-like Kinase (PLK)
|
Cancer
|
Poloxime, a hydrolysis product of poloxin, is a non-ATP-competitive Plk1 inhibitor, with moderate Plk1 inhibitory activity.
|
-
- HY-N2115
-
Chikusetsusaponin IV
|
Renin
|
Cardiovascular Disease
|
Araloside A (Chikusetsusaponin IV) is a component of Panax japonicus, with low-renin-inhibitory activity, with an IC50 of 77.4 μM .
|
-
- HY-N4258
-
|
Glucosidase
|
Metabolic Disease
|
Panasenoside is a flavonoid isolated from Lilium pumilum DC. Panasenoside exhibits α-glucosidase inhibitory activity .
|
-
- HY-N2053
-
-
- HY-N8215
-
|
Others
|
Metabolic Disease
|
Achyranthoside C is a saponin from Achyranthes bidentata. The derivative of Achyranthoside C has inhibitory activity on osteoclast formation .
|
-
- HY-115714
-
|
CDK
|
Cancer
|
CDK9-IN-12 displays the optimal CDK9 inhibitory activity with an IC50 value of 5.41 nM.
|
-
- HY-139713
-
|
Fungal
|
Infection
|
Antifungal agent 14 exhibits broad-spectrum activity against the fungal strains with excellent minimum inhibitory concentration values.
|
-
- HY-N8469
-
-
- HY-122953
-
|
COX
|
Inflammation/Immunology
|
Daturaolone is a natural triterpenoid with anti-inflammatory and antinociceptive potentials. Daturaolone displays a COX-1 inhibitory activity .
|
-
- HY-N0493
-
|
COX
Lipoxygenase
|
Inflammation/Immunology
|
Pectolinarigenin is a dual inhibitor of COX-2/5-LOX. Anti-inflammatory activity . Pectolinarigenin has potent inhibitory activities on melanogenesis .
|
-
- HY-114651
-
|
Others
|
Cancer
|
Phenazoviridin is a free radical scavenger. Phenazoviridin shows strong inhibitory activity against lipid peroxidation in rat brain homogenate and exhibits antihypoxic activity in mice .
|
-
- HY-126740
-
|
Antibiotic
Fungal
|
Infection
Cancer
|
Anguinomycin A is an antibiotic that exhibits good inhibitory activity against G. boninense with an MIC value of 5 µg/disk. Anguinomycin A has antitumor activity .
|
-
- HY-114313
-
|
Microtubule/Tubulin
|
Cancer
|
Microtubule inhibitor 1 is an antitumor agent with microtubule polymerization inhibitory activity, with an IC50 value of 9-16 nM in cancer cells .
|
-
- HY-W009417
-
|
Glucosidase
|
Metabolic Disease
|
Cedryl acetate is a tricyclic sesquiterpene isolated from the plant Cunninghamia lanceolata. Cedryl acetate shows α-glucosidase inhibitory activity .
|
-
- HY-N9513
-
-
- HY-N4230
-
|
COX
|
Inflammation/Immunology
|
Clematomandshurica saponins B shows significant inhibitory activity on cyclooxygenase-2 (IC50=2.58 mM) .
|
-
- HY-N10224
-
|
Acyltransferase
|
Metabolic Disease
|
Terpendole C, produced by Albophoma yamanashiensis, shows potent inhibitory activity against acyl-CoA: cholesterol acyltransferase (ACAT) .
|
-
- HY-117601
-
|
Others
|
Inflammation/Immunology
|
11-Deoxyalisol B, a triterpene, shows the potent inhibitory activity on Lipopolysaccharide (LPS)-induced nitric oxide (NO) production .
|
-
- HY-N10641
-
|
Others
|
Cancer
|
Epinodosinol is a diterpenoid derived from plant Rabdosia angustifolia. Epinodosinol has inhibitory activity against certain cancer cells .
|
-
- HY-137011
-
|
COX
|
Others
|
3,9-Dihydroeucomin (compound 12) is a natural homoisoflavonoid compound with less COX-2 inhibitory activitys .
|
-
- HY-N12472
-
|
Aldose Reductase
|
Others
|
Floramanoside C shows 2,2-diphenyl-1-picrylhydrazyl scavenging and aldose reductase inhibitory activities .
|
-
- HY-B0984A
-
|
STING
|
Infection
Cancer
|
Fendiline is a STING agonist and has tumor growth inhibitory activity. Fendiline can be used for research on cancer and viral infections .
|
-
- HY-108161
-
|
Interleukin Related
|
Others
|
LF 1695 is an immunomodulator. LF 1695 enhances the proliferative response of T cells by increasing the production of IL2 (interleukin-2) or the expression of the IL2 receptor. LF 1695 also increases CONA-induced inhibitory activity in human lymphocytes. LF 1695 can be used to study the proliferative and inhibitory activity of T cell subpopulations, as well as their role in immune regulation .
|
-
- HY-13561
-
M475271
|
Src
|
Cancer
|
AZM475271 is a potent and selective Src kinase inhibitor with IC50 of 5 nM; no inhibitory activity on Flt3, KDR, Tie-2.
|
-
- HY-N6890
-
|
Others
|
Metabolic Disease
|
Tarasaponin VI is a natural product isolated from Aralia elata. Tarasaponin VI shows potent inhibitory activity on ethanol absorption .
|
-
- HY-131114
-
|
Others
|
Others
|
Valiolamine is an aminocyclitol. Valiolamine has potent alpha-glucosidase inhibitory activity against porcine intestinal sucrase, maltase and isomaltase .
|
-
- HY-N5063
-
-
- HY-19041
-
-
- HY-105027
-
-
- HY-160983
-
|
DNA/RNA Synthesis
|
Cancer
|
PHYLPA-8 is an inhibitor for DNA polymerase-α, which exhibits weak inhibitory activity for the stereochemistry of the fatty acid moiety and the cyclic phosphate .
|
-
- HY-14874
-
FYX-051
|
Xanthine Oxidase
Cytochrome P450
|
Metabolic Disease
|
Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment .
|
-
- HY-N12134
-
|
Monoamine Oxidase
|
Neurological Disease
|
Methylpiperic acid is a piperine alkaloid with significant MAO inhibitory activity (IC503.6 μM). Methylpiperic acid is less effective against MAO-B (IC 501.6 μM) than MAO-A (IC5027.1 μM) has a bidirectional inhibitory effect. Methylphenidate is used to treat mental disorders .
|
-
- HY-105463
-
|
Antibiotic
Bacterial
|
Infection
Cancer
|
Saptomycin D is an antibiotic with antitumor activity isolated from the Streptomyces sp. HP530 strain. Saptomycin D exhibits potent inhibitory effects against Gram-positive bacteria, while demonstrating weaker inhibitory activities against certain Gram-negative bacteria and yeasts. Saptomycin D also displays remarkable antitumor properties. Saptomycin D is applicable in research within the field of oncology .
|
-
- HY-130787
-
|
NO Synthase
|
Inflammation/Immunology
|
Apterin is a natural compound with anti-inflammatory activity. Apterin shows significantly inhibitory activity on NO production in RAW264.7 cells with an IC50 value of 41.8 μM .
|
-
- HY-121020
-
|
Phosphatase
|
Neurological Disease
|
Arcapillin is a flavonoid that can be isolated from Artemisia capillaris Thunb. Arcapillin has antispasmodic activity. Arcapillin also has moderate PTP1B inhibitory activity .
|
-
- HY-N10192
-
|
Endogenous Metabolite
Bacterial
|
Infection
|
Aculene D, a fungal metabolite, shows quorum sensing (QS) inhibitory activity against Chromobacterium violaceum CV026, and could significantly reduce violacein production in N-hexanoyl-l-homoserine lactone (C6-HSL) induced C. violaceum CV026 cultures at sub-inhibitory concentrations .
|
-
- HY-161124
-
|
Bacterial
|
Infection
|
Antibacterial agent 175 (compound Y40), a ML346 (HY-18669) analog, is a Sortase A (SrtA) inhibitor. Antibacterial agent 175 shows inhibitory activity on Staphylococcus aureus SrtA and shows inhibitory effects on biofilm formation. Antibacterial agent 175 is an antivirulence agent against S. aureus infections .
|
-
- HY-N9314
-
-
- HY-N8024
-
|
TMV
|
Infection
|
Rubinaphthin A is a naphthohydroquinone that can be found in the roots of Rubia yunnanensis. Rubinaphthin A exhibits inhibitory activity against tobacco mosaic virus (TMV) .
|
-
- HY-N9528
-
-
- HY-W001023
-
5A8HQ
|
Proteasome
|
Cancer
|
5-Amino-8-hydroxyquinoline (5A8HQ), a potential anticancer candidate, has promising proteasome inhibitory activity.
|
-
- HY-126455
-
Vermixocin A
|
Acyltransferase
|
Metabolic Disease
|
Penicillide (Vermixocin A), isolated from Talaromyces derxii cultivated on rice, shows inhibitory activity against acyl-CoA:cholesterol acyltransferase (ACAT) .
|
-
- HY-N1158
-
|
Others
|
Others
|
Tinospinoside C is a bioactive?clerodane diterpene glycoside compound. Tinospinoside C shows inhibitory activities of NO production with an IC50 value of 218 μM .
|
-
- HY-N12262
-
|
Bacterial
|
Infection
Cancer
|
(+)-Epieudesmin is an antineoplastic agent. (+)-Epieudesmin has marginal cancer cell line inhibitory activities. (+)-Epieudesmin inhibits the growth of Gram-negative pathogen .
|
-
- HY-N5075
-
|
Others
|
Neurological Disease
|
Quercetin 3-O-glucoside-7-O-rhamnoside is a member of flavonoid glycosides group with an inhibitory activity on the CNS .
|
-
- HY-75680
-
|
Factor Xa
|
Cardiovascular Disease
|
FaX-IN-1 (compound 11A) is an intermediate in the preparation of FaX inhibitors and was used to study the inhibitory activity against venous thrombosis in rats .
|
-
- HY-N2266
-
|
COX
|
Inflammation/Immunology
|
Benzoylgomisin O isolated from Schisandra rubriflora, has inhibitory activity against 15-LOX, COX-1 and COX-2 enzymes and anti-inflammatory activity .
|
-
- HY-N10448
-
|
TNF Receptor
|
Inflammation/Immunology
|
Sinulatumolin E (compound 6), a terpenoid, displays significant TNF-α inhibitory activity with an IC50 of 3.6 μM. Sinulatumolin E (compound 6) exhibits anti-inflammatory activity .
|
-
- HY-114336
-
|
Phosphatase
|
Inflammation/Immunology
|
Enocyanin is an anthocyanin extracted from grapes. Enocyanin shows inhibitory effect on the leucine aminopeptidase, acid phosphatase, γ-glutamyl transpeptidase and esterase activity .
|
-
- HY-Y0790
-
p-Isopropylbenzaldehyde
|
Endogenous Metabolite
|
Cancer
|
Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity .
|
-
- HY-N9317
-
|
Glucosidase
|
Metabolic Disease
|
Tangshenoside I, isolated from the roots of Codonopsis lanceolata, exhibits weak α-glucosidase inhibitory activities in vitro with an IC50 of 1.4 mM .
|
-
- HY-N8184
-
-
- HY-139622
-
|
Others
|
Others
|
DN-F01 has a strong inhibitory calcium-dependent effect on cardiac myofibrillar ATPase activity with an IC50 value of 11 ± 4 nmol/L.
|
-
- HY-N12263
-
|
Amylases
|
Metabolic Disease
|
3,5,6,7,8,4'-Hexamethoxyflavone is a inhibitor of α-Amylase with the inhibitory activity of 28.3% at 500 μM .
|
-
- HY-N11965
-
-
- HY-N12361
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
Osmanthuside B can be isolated from Pseuderanthemum carruthersii (Seem.) Guill. var. atropurpureum (Bull.) Fosb and has weak acetylcholinesterase inhibitory activity .
|
-
- HY-163204
-
|
P-glycoprotein
|
Cancer
|
RhQ-DMB is a potent inhibitor of P-gp. RhQ-DMB exhibits high affinity and inhibitory activity in yeast strains expressing CmABCB1 .
|
-
- HY-N12398
-
|
Others
|
Neurological Disease
|
Psychotridine is a natural alkaloid isolated from Psychotria colorata, reveals an analgesic activity in nervous system and an inhibitory efficacy towards platelet aggregation .
|
-
- HY-N8535
-
|
Bacterial
|
Infection
|
Massarigenin C is a compound that can be isolated from Massarina tunicata. Massarigenin C has inhibitory activity against Bacillus subtilis (ATCC 6051) .
|
-
- HY-125732
-
|
Others
|
Infection
|
Decarestrictine D exhibits inhibitory activity against cholesterol levels. Decarestrictine D is utilized as receptor for glycosylation reactions to synthesize novel hybrid antibiotics .
|
-
- HY-N8018
-
-
- HY-15508
-
JANEX-1
4 Publications Verification
WHI-P131; Jak3 inhibitor I
|
JAK
|
Cancer
|
JANEX-1 (WHI-P131) is a potent and specific JAK3 inhibitor (estimated Ki=2.3 μM). JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC50 of 78 μM), does not inhibit JAK1 and JAK2.
|
-
- HY-N2039
-
|
Others
|
Cancer
|
20(R)-Ginsenoside Rg2 shows inhibitory effects on lung cancer NCI-H1650 cells. Anti-cancer activities .
|
-
- HY-N8209
-
-
- HY-145357
-
|
SGLT
|
Metabolic Disease
|
SGLT1/2-IN-2 demonstrates potent dual inhibitory activities (IC50 = 96 nM for SGLT1 and IC50 = 1.3 nM for SGLT2).
|
-
- HY-N3643
-
|
Others
|
Cancer
|
Cryptomeridiol can be isolated from Phaulopsis imbricata. Cryptomeridiol has melanogenesis inhibitory activity in the α-MSH-stimulated B16 melanoma cells .
|
-
- HY-P10159
-
|
Bacterial
|
Infection
|
Diplacol ia a natural compound from from Mimulus clevelandi and shows potent inhibitory activities against lipopolysaccharide (LPS)-induced nitric oxide production .
|
-
- HY-N12511
-
|
nAChR
|
Neurological Disease
|
Aristoquinoline (Compound 1) is an alkaloid can be isolated from Aristotelia chilensis. Aristoquinoline has α3β4 nAChR inhibitory activity .
|
-
- HY-N0616
-
|
Tyrosinase
|
Inflammation/Immunology
Cancer
|
Trifolirhizin is a pterocarpan flavonoid isolated from the roots of Sophora flavescens. Trifolirhizin possesses potent tyrosinase inhibitory activity with an IC50 of 506 μM . Trifolirhizin exhibits potential anti-inflammatory and anticancer activities .
|
-
- HY-114798
-
-
- HY-N2010
-
-
- HY-B0125
-
-
- HY-119821
-
|
Glucosidase
|
Infection
|
Terphenyllin is a naturally abundant p-terphenyl metabolite isolated from the coral derived fungus Aspergillus candidus, has significant α-glucosidase inhibitory activity .
|
-
- HY-N1547
-
-
- HY-N10453
-
|
TNF Receptor
|
Inflammation/Immunology
|
Sinulatumolin D (compound 4) is an anti-inflammatory agent. Sinulatumolin D has significant TNF-α inhibitory activity with an IC50 value of 5.5 μM .
|
-
- HY-N10454
-
|
TNF Receptor
|
Inflammation/Immunology
|
Sinulatumolin C (compound 3) is an anti-inflammatory agent. Sinulatumolin C has significant TNF-α inhibitory activity with an IC50 value of 2.6 μM .
|
-
- HY-108877
-
BMY-28142 hydrochloride
|
Antibiotic
Bacterial
|
Infection
|
Cefepime hydrochloride is a cephalosporin antibiotic agent. Cefepime hydrochloride has inhibitory activity against human serum paraoxonase-1 (hPON1) with an IC50 value of 21.115 mM .
|
-
- HY-N8619
-
|
Others
|
Cancer
|
Minimolide F is a sesquiterpene lactone. Minimolide F has inhibitory activity against human nasopharyngeal cancer cells. Minimolide F can be used for the research of cancer .
|
-
- HY-146212
-
|
HDAC
HSP
|
Cancer
|
These compounds have strong hdac and hsp90 inhibitory activities. Compound 20 (HDAC ic50 = 194 nm; Hsp90 α < b> Ic50 = 153 nm) and compound 26 ((HDAC ic50= 360 nm; Hsp90 α < b> Ic50 = 77 nm) shows the strongest HDAC and HSP90 α Inhibitory activity. Both compounds can induce hsp90 expression and down regulate hsp90 client proteins, which play an important role in regulating the survival and invasion of cancer cells.
|
-
- HY-119458
-
|
Topoisomerase
TMV
Fungal
|
Infection
|
Luotonin A is an antiviral and antiphytopathogenic fungus agent. Luotonin A has good antiviral activity against tobacco mosaic virus (TMV). Luotonin A also has certain inhibitory activity on topoisomerase I and topoisomerase II. Luotonin A shows antitumor activity .
|
-
- HY-131069A
-
|
Influenza Virus
|
Infection
|
MBX2329, a potent influenza virus inhibitor, specifically inhibits hemagglutinin (HA)-mediated viral entry with HIV/HA(H5) displaying IC90 of 8.6 μM. MBX2329 inhibits a wide spectrum of influenza A viruses, which includes the 2009 pandemic influenza virus A/H1N1/2009, highly pathogenic avian influenza (HPAI) virus A/H5N1, and oseltamivir-resistant A/H1N1 strains .
|
-
- HY-N8092
-
|
Phosphodiesterase (PDE)
|
Infection
Inflammation/Immunology
|
Kushenol B is an isoprenoid flavonoid isolated from S. flavescens, has antimicrobial, anti-inflammatory and antioxidant activities . Kushenol B has inhibitory activity against cAMP phosphodiesterase (PDE), with an IC50 of 31 µM .
|
-
- HY-141844
-
|
HDAC
|
Cancer
|
HDAC/BET-IN-1 displays submicromolar inhibitory activity against HDAC1 and 6 (IC50 = 0.163 μM and 0.067 μM), and BRD4 (Ki = 0.076 μM), and possess potent antileukemia activity.
|
-
- HY-146330
-
|
Bacterial
|
Infection
|
FtsZ-IN-2 (Compound 19) is an inhibitor of the bacterial cell division protein FtsZ with GTPase inhibitory activity. FtsZ-IN-2 exhibits anti-staphylococcal activity with MIC values of 2 µg/ml for MSSA and MRSA .
|
-
- HY-151875
-
|
Bacterial
|
Infection
Inflammation/Immunology
|
MurA-IN-3 is a reversible pyrrolidinedione-based MurA inhibitor. MurA-IN-3 has inhibitory activity for MurA with an IC50 value of 4.5 μM. MurA-IN-3 also has antibacterial activity .
|
-
- HY-14874S
-
FYX-051-d4
|
Isotope-Labeled Compounds
Xanthine Oxidase
Cytochrome P450
|
Metabolic Disease
|
Topiroxostat-d4 is deuterium labeled Topiroxostat. Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment[1][2].
|
-
- HY-164051
-
|
Bacterial
|
Infection
|
1650-M15 is an inhibitor of lipoteichoic acid synthase (LtaS). It has inhibitory activity against Gram-positive bacteria but has no significant inhibitory effect against Gram-negative bacteria. The IC50s of 1650-M15 against MRSA and MSSA are 62.44 μM and 66.42 μM, respectively, and the MICs are both 200 μM .
|
-
- HY-B0222
-
Behenyl alcohol
|
HSV
|
Infection
|
1-Docosanol (Behenyl alcohol) is a saturated fatty alcohol with reported inhibitory activity against lipid-enveloped viruses, including herpes simplex virus (HSV) .
|
-
- HY-U00157
-
W2395; NSC297623
|
Others
|
Inflammation/Immunology
|
Meseclazone (W2395;NSC297623) exhibits inhibitory potency of secondary phase ADP aggregation. Meseclazone possesses anti-inflammatory, analgesic and antipyretic activity.
|
-
- HY-N0555
-
|
Others
|
Metabolic Disease
|
Escin IB is a saponin isolated from skin and the endosperm of seeds of horse chestnut (Aesculus hippocastanum). Escin IB shows inhibitory effect on pancreatic lipase activity .
|
-
- HY-N7203
-
|
Glucosidase
|
Metabolic Disease
|
N-Caffeoyl O-methyltyramine is a class of alkaloid isolated from Cuscuta reflexa with strong inhibitory activity against α-glucosidase (IC50 of 103.58 μM) .
|
-
- HY-N2058
-
|
Bacterial
Apoptosis
|
Infection
Cancer
|
Neogambogic acid, an active ingredient in garcinia, induces apoptosis and has anticancer effect. Neogambogic acid has significant inhibitory activity toward methicillin-resistant Staphylococcus aureus (MRSA) .
|
-
- HY-N4136
-
|
Bacterial
Apoptosis
Endogenous Metabolite
|
Infection
|
Lonicerin is an anti-algE (alginate secretion protein) flavonoid with inhibitory activity for P. aeruginosa. Lonicerin prevents inflammation and apoptosis in LPS-induced acute lung injury .
|
-
- HY-N6621
-
|
Topoisomerase
|
Cancer
|
Hippeastrine, an active alkaloid, exhibits a good dose-dependent inhibitory effect against topoisomerase I (Top I) with an IC50 at 7.25 μg/mL. Antiproliferative and anticancer activities .
|
-
- HY-101404S
-
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Others
|
DL-Homocysteine thiolactone-d4 hydrochloride is the deuterium labeled DL-Homocysteine thiolactone (hydrochloride). DL-Homocysteine thiolactone hydrochloride is a cyclic amino acid derivative that exhibits root-growth inhibitory activity.
|
-
- HY-N4168A
-
5-O-Caffeoylquinic acid methyl ester
|
HBV
|
Infection
Cancer
|
Neochlorogenic acid methyl ester (5-O-Caffeoylquinic acid methyl ester) is an HBV inhibitor. Neochlorogenic acid methyl ester can be isolated from L. japonica flower buds with potent HBV inhibitory activity .
|
-
- HY-155094
-
|
DNA/RNA Synthesis
|
Others
|
DNA polymerase-IN-3 (Compd 5b) is a coumarin derivative that exhibits inhibitory activity against Taq DNA polymerase and can be used in proliferative disease research .
|
-
- HY-P5107
-
|
VEGFR
|
Cancer
|
Protein LMWP is a cell-penetrating peptide with vascular endothelial growth factor (VEGF) inhibitory activity. Protein LMWP can inhibit tumor growth and is used in cancer research .
|
-
- HY-126983
-
Epoxybergamottin
|
Others
|
Others
|
6',7'-Epoxybergamottin is a metabolism of Penicillium digitatum. 6',7'-Epoxybergamottin can be used in study the cytochrome P450 3A4 inhibitory activity .
|
-
- HY-N12600
-
|
Bacterial
|
Infection
|
Thiolopyrrolone A (compound 1) exhibits antibacterial activities against BCG, M. tuberculosis and S. aureus with minimum inhibitory concentrations (MIC) of 10, 10 and 100 μg/mL, respectively .
|
-
- HY-N12737
-
|
Others
|
Inflammation/Immunology
|
15-epi-Danshenol A is a diterpenoid with an immune-modulating activity. 15-epi-Danshenol A shows inhibitory effect on B lymphoblasts cells in a concentration-dependent manner .
|
-
- HY-100385
-
Cyclo(L-Pro-L-Trp)
|
PI3K
Bacterial
|
Infection
|
Brevianamide F (Cyclo(L-Pro-L-Trp)) is a mycotoxin isolated from Colletotrichum gloeosporioides, with antibacterial activity. Brevianamide F shows potent PI3Kα inhibitory activity with an IC50 of 4.8 µM .
|
-
- HY-W001542
-
-
- HY-N6310
-
|
Bacterial
|
Infection
|
Talaromycesone A is an oxaphenalenone dimer compound. Talaromycesone A exhibits potent antibacterial activities with an IC50 of 3.70 μM, against human pathogenic Staphylococcus strains. Talaromycesone A displays potent acetylcholinesterase inhibitory activities with an IC50 of 7.49 μM .
|
-
- HY-N9535A
-
|
Drug Metabolite
|
Metabolic Disease
|
(R)-tert-OMe-byakangelicin is a kind of furanocoumarin, which has inhibitory activity to liver drug metabolizing enzyme (DME) activity. (R)-tert-OMe-byakangelicin can be isolated from immature fruits of Angelica sinensis .
|
-
- HY-N7346
-
|
HSV
Cholinesterase (ChE)
|
Infection
|
Lucidadiol is a natural compound isolated from Ganoderma lucidum. Lucidadiol exhibits acetylcholinesterase-inhibitory activity, with IC50 values of 31 μM. Lucidadiol shows antiviral activity against influenza virus type A and HSV type 1 .
|
-
- HY-N0136
-
(+)-Dihydroquercetin; (+)-Taxifolin
|
Autophagy
Tyrosinase
|
Inflammation/Immunology
|
Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
|
-
- HY-10393
-
PNU-100592
|
Bacterial
Antibiotic
|
Infection
|
Eperezolid(PNU-100592) is a oxazolidinone antibacterial agent, Eperezolid demonstrated good in vitro inhibitory activity, regardless of methicillin susceptibility for staphylococci(MIC90= 1-4 mg/ml).
|
-
- HY-20349
-
|
Bacterial
|
Infection
|
Monobehenin, an bacterial biofilm formation inhibitor, has strong inhibitory activity toward bacterial biofilm formation of S. mutans, X. oryzae, and Y. enterocolitica in a strain specific manner .
|
-
- HY-N0893S
-
-
- HY-N7989
-
Tellimoside
|
Others
|
Others
|
Quercetin 3-O-(6''-O-galloyl)-β-D-glucoside (Tellimoside) is a flavonol glycoside with strong inhibitory activity against the growth of Microcystis aeruginosa .
|
-
- HY-N10128
-
|
Bacterial
|
Infection
|
(8'α,9'β-Dihydroxy)-3-farnesylindole shows strong inhibitory activity (EC50 9.8 μM) against B. subtilis.
|
-
- HY-144236
-
|
Epigenetic Reader Domain
|
Others
|
Considerable studies confirmed that BRD4 inhibition ameliorated kidney injury and fibrosis ,and ZLD2218 exhibited the most potent inhibitory activity against BRD4, with the IC50 value of 107 nM
|
-
- HY-N10275
-
|
Others
|
Inflammation/Immunology
|
Herpotrichone A shows potent anti-neuroinflammatory activity in lipopolysaccharide (LPS)-induced BV-2 microglial cells with the half maximal inhibitory concentration (IC50) value of 0.41 μM.
|
-
- HY-123922
-
|
Bacterial
|
Infection
|
NOSO-502 is an inhibitor of bacterial translation. NOSO-502 exhibits inhibitory activity against Enterobacteriaceae. NOSO-502 has good safety and antibacterial properties .
|
-
- HY-N3674
-
|
TGF-beta/Smad
|
Inflammation/Immunology
|
Dalbergioidin, a well-known anthocyanin, ameliorates doxorubicin-induced renal fibrosis by suppressing the TGF-β signal pathway. Dalbergioidin exhibits tyrosinase inhibitory activity with an IC50 of 20 mM .
|
-
- HY-N3091
-
|
Tyrosinase
|
Others
|
Persiconin is a tyrosinase Inhibitor. Persiconin can be isolated from Prunus persica. Persiconin has tyrosinase inhibitory activity of 46% at 500 μM. Persiconin can be used in whitening research .
|
-
- HY-N9036
-
|
Influenza Virus
|
Infection
|
Drechslerine A has neuraminidase inhibitory activity (IC50: 0.79 μM). Drechslerine A is a terpene that can be isolated from endophytic Cochliobolus. Drechslerine A can be used for research of Influenza Virus .
|
-
- HY-W354851
-
|
Bacterial
Antibiotic
|
Infection
|
Pisiferic acid is an antibacterial agent with inhibitory activity against Gram-negative/positive bacteria such as P. vulgaris, S. aureus and B. subtilis. Pisiferic acid can be used to study bacterial infections .
|
-
- HY-163109
-
|
Carbonic Anhydrase
|
Infection
|
Carbonic anhydrase inhibitor 16 (compound 1) is a dengue protease inhibitor with inhibitory activity against carbonic anhydrase hCA I and hCA II (Ki: 28.5 nM, 2.2 nM) .
|
-
- HY-N12618
-
|
Proteasome
|
Others
|
Crocapeptin C is a cyclic depsipeptide that can be extrated from Melittangium boletus. Crocapeptin C exhibits potent inhibitory activity against chymotrypsin with an IC50 value of 0.5 µM .
|
-
- HY-161396
-
-
- HY-P10447
-
Fengycin IX; SNA-60-367-3
|
Phospholipase
|
Inflammation/Immunology
|
Plipastatin A1 is a lipopeptide with enzyme inhibitory and immunosuppressive activities. Plipastatin A1 is found in Bacillus cereus and inhibits phospholipase A2 (PLA2), PLC, and PLD .
|
-
- HY-158257
-
|
Fluorescent Dye
|
Others
|
Firefly luciferase-IN-4 (CID: 3987260) is an inhibitor of ATP-dependent luciferase (Firefly luciferase). It has nM-level inhibitory activity (pIC< sub>50=6.5) .
|
-
- HY-138100
-
(+)-Hyalodendrin
|
Fungal
|
Infection
|
Hyalodendrin ((+)-Hyalodendrin) is a fungal growth inhibitor with inhibitory activity against wood decay fungi. Hyalodendrin has low phytotoxicity, with an acute toxicity (LD50) of 75 mg/kg in mice .
|
-
- HY-14874R
-
|
Xanthine Oxidase
Cytochrome P450
|
Metabolic Disease
|
Topiroxostat (Standard) is the analytical standard of Topiroxostat. This product is intended for research and analytical applications. Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment .
|
-
- HY-15517B
-
|
Others
|
Cancer
|
KN-92 hydrochloride is an inactive derivative of KN-93, without CaM kinase inhibitory activity. KN-92 hydrochloride is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93 .
|
-
- HY-107981
-
|
Antifolate
|
Cancer
|
LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity .
|
-
- HY-122289
-
|
Dihydrofolate reductase (DHFR)
Bacterial
|
Infection
|
Metioprim is a competitive inhibitor of bacterial Dihydrofolate reductase (DHFR). Metioprim has inhibitory activity against anaerobic bacteria. Metioprim shows synergistic activity in combination with DDS (HY-B0688) against E. coli. and various mycobacteria .
|
-
- HY-100659
-
PCI-45227
|
Btk
|
Cancer
|
Dihydrodiol-Ibrutinib (PCI-45227) is a dihydrodiol active metabolite of Ibrutinib (HY-10997), has inhibitory activity towards BTK approximately 15 times lower than that of ibrutinib .
|
-
- HY-B0502A
-
BAY Vp 2674 monohydrochloride; PD160788 monohydrochloride
|
Bacterial
Antibiotic
Endogenous Metabolite
Orthopoxvirus
|
Infection
|
Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis. Enrofloxacin monohydrochloride shows inhibitory activity against vaccinia virus (VV).
|
-
- HY-N10274
-
-
- HY-N10285
-
|
Tyrosinase
|
Infection
|
Phaeosphaone D is a thiodiketopiperazine alkaloid compound isolated from Phaeosphaeria fuckelii, an endophytic fungus. Phaeosphaone D displays mushroom tyrosinase inhibitory activity with an IC50 value of 33.2 μM .
|
-
- HY-N11552
-
|
Glutathione Peroxidase
|
Inflammation/Immunology
|
Sorbifolin, a flavone glucoside, can be isolated from the Pterogyne nitens. Sorbifolin has myeloperoxidase inhibitory and radical scavenging activities. Sorbifolin is also a MPO inhibitor with an IC50 value of 19.2 nM .
|
-
- HY-Y0729
-
|
Tyrosinase
Bacterial
Fungal
|
Infection
|
4-Chlorocinnamic acid has inhibitory effects on tyrosinase. 4-Chlorocinnamic acid has antibacterial activity. 4-Chlorocinnamic acid also inhibits Colletotrichum gloeosporioides growth .
|
-
- HY-N11940
-
|
HIV Protease
|
Infection
|
Acetyl-binankadsurin A (compound 5) is a lignan isolated from Kadsura longipedunculata. Acetyl-binankadsurin A has low inhibitory activity against HIV-1 protease, with IC50 >100 μg/mL .
|
-
- HY-N11993
-
|
Cholinesterase (ChE)
|
Others
|
Aloveroside A is a triglucosylnaphthalene derivative isolated from ethanolic extract of aloe vera. Aloveroside A has weak bACE inhibitory activity (inhibition rate at a dose of 100 μg/mL is approximately 18.68%) .
|
-
- HY-N12636
-
|
Parasite
|
Infection
|
Kagimminols A is a cembrene-type diterpenoids and can be isolated from an Okeania sp. marine cyanobacterium. Kagimminols A shows selective growth-inhibitory activity against the causative agent of human African trypanosomiasis .
|
-
- HY-161333
-
-
- HY-100338
-
|
Btk
|
Cancer
|
CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn .
|
-
- HY-115770
-
|
Bacterial
|
Inflammation/Immunology
|
8-Methylsulfinyloctyl isothiocyanate, an isothiocyanate, has antimicrobial activity and remarkable inhibitory activity against plant growth . 8-Methylsulfinyloctyl isothiocyanate impair COX-2 mediated inflammatory responses in LPS stimulated raw macrophages .
|
-
- HY-N0136A
-
(±)-Dihydroquercetin
|
Autophagy
Tyrosinase
|
Inflammation/Immunology
|
(±)-Taxifolin ((±)-Dihydroquercetin) is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
|
-
- HY-33900
-
3-Oxotetrahydrofuran
|
Others
|
Others
|
Dihydrofuran-3(2H)-one (3-Oxotetrahydrofuran) can be used to synthesize cyclic ketone inhibitors that inhibit the serine protease plasmin and increase its inhibitory activity .
|
-
- HY-136498
-
|
Drug Metabolite
|
Infection
|
T-705RMP, a phosphorylated metabolite of T-705, exhibits a very weak inhibitory effect on the IMP dehydrogenase (IMPDH) activities of the host cells, with an IC50 of 601 μM .
|
-
- HY-N9324
-
|
Xanthine Oxidase
|
Inflammation/Immunology
|
Ilexoside O is a triterpene saponin isolated from the roots of Ilex pubescens. Ilexoside O exhibits weak xanthine oxidase (XOD) inhibitory activity (IC50=53.05 μM) .
|
-
- HY-W047478
-
NSC 10154
|
Others
|
Cancer
|
3-Methylcarbazole is an carbazole alkaloid compound with anticancer effects. 3-Methylcarbazole shows growth inhibitory activity (IC50 of 25 μg/mL) on human fibrosarcoma HT-1080 cells .
|
-
- HY-115930
-
|
Bcl-2 Family
|
Cardiovascular Disease
|
Bim-IN-1 is a potent Bim expression inhibitor. Bim-IN-1 reduces Bim expression levels and has little inhibitory effect upon protein kinase A activity and minimal toxicity .
|
-
- HY-143436
-
|
Others
|
Cancer
|
TNIK-IN-4 is a potent TNIK inhibitor with IC50 of 0.61 μM. TNIK-IN-4 has inhibitory activity against typical colorectal cancer cell line HCT116 .
|
-
- HY-128424
-
|
Others
|
Metabolic Disease
|
4'-Deoxyphlorizin is an inhibitor of the glucose transport system. 4'-Deoxyphlorizi has good phlorizin hydrolase inhibitory activity with the Km value of 0.59 nM and the Ki value of 0.33 nM, respectively .
|
-
- HY-N8669
-
|
LIM Kinase (LIMK)
|
Cancer
|
Curcolonol is a furan type sesquiterpene. Curcolonol can be isolated from several medical herbs. Curcolonol has inhibitory activity for LIM kinase 1. Curcolonol can be used for the research of breast cancer .
|
-
- HY-P3985
-
Bradykinin potentiating peptide B
|
Angiotensin-converting Enzyme (ACE)
|
Others
|
Bradykinin potentiator B (Bradykinin potentiating peptide B) is venom of Agkistrodon halys blomhoffi. Bradykinin potentiator B is a potent ACE inhibitor. Bradykinin potentiator inhibits the activity of bradykinin inhibitory peptidase .
|
-
- HY-120711
-
ML187
|
Apoptosis
|
Metabolic Disease
|
BRD0476 is an inhibitor of pancreatic β-cell apoptosis with an EC50 value of 0.78 μM and a maximal inhibitory activity of 99%. BRD0476 can be used in diabetes-related research .
|
-
- HY-123886
-
|
Others
|
Cancer
|
Aranciamycin (Compound 1) is an anthracycline antibiotic with collagenase inhibitory activity (IC503.7*10-7M). Aranciamycin can be used to inhibit DNA synthesis in tumor cells .
|
-
- HY-N8984
-
|
Others
|
Others
|
Kanshone B (Compound 5) is isolated from the
natural Nardostachys chinensis. Kanshone B shows inhibitory
activity against LPS-induced NO production (IC50=11.5 μM)
.
|
-
- HY-N3574
-
|
Fungal
|
Infection
|
Chloramultilide B is a lindenane dimer that can be isolated from Chloranthus serratus. Chloramultilide B has inhibitory activities against Candida albicans and C.parapsilosis with a MIC value of 0.068 μM .
|
-
- HY-400902
-
|
YAP
|
Cancer
|
YAP/TAZ inhibitor-3 (Compound 24) is a YAP/TAZ inhibitor. YAP/TAZ inhibitor-3 shows firefly luciferase inhibitory activity, with an IC50 < 0.1 μM .
|
-
- HY-121294
-
X 14547A
|
Others
|
Infection
|
Indanomycin is an antibiotic of the pyrroloketoindane class, which includes an unusual indane ring structure. It has bactericidal activity against Gram-positive bacteria, with minimum inhibitory concentration (MIC) values of ≤0.2 μg/mL.
|
-
- HY-160870
-
|
Fluorescent Dye
|
Others
|
Firefly luciferase-IN-3 (CID: 17087944) is an inhibitor of ATP-dependent luciferase (Firefly luciferase) and has nM-level inhibitory activity against NanoLuc (pIC50=7.5) .
|
-
- HY-N0136B
-
(-)-Dihydroquercetin
|
Tyrosinase
|
Inflammation/Immunology
|
(-)-Taxifolin is the less active enantiomer of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
|
-
- HY-N3518
-
|
Tyrosinase
|
Metabolic Disease
|
Mulberroside F is one of the main bioactive constituents in mulberry (Morus alba L.) . Mulberroside F shows inhibitory effects on tyrosinase activity and on the melanin formation. Mulberroside F also exhibits superoxide scavenging activity that is involved in the protection against auto-oxidation .
|
-
- HY-19936
-
|
Bacterial
|
Infection
|
ACHN-975 is a selective LpxC inhibitor and exhibits a subnanomolar LpxC inhibitory activity. ACHN-975 is against a wide range of gram-negative bacterias with low MIC values (≤1 μg/mL) .
|
-
- HY-126237
-
|
Fungal
|
Infection
|
Acetyllovastatin, a acetate of Lovastatin, presentes a moderate inhibitory effect against the enzyme acetylcholinesterase with an IC50 of 79 μg/mL. Lovastatin has been found to display antifungal activity, and suppresses proliferation of a number of transformed cell lines .
|
-
- HY-B1144A
-
Clomidazole hydrochloride
|
Fungal
|
Infection
|
Chlormidazole hydrochloride is an antifungal agent and has inhibitory activity against many fungi and some gram-positive cocci. Chlormidazole hydrochloride can be applied in fungal and bacterial infections of nails and skin, including interdigital and periungual mycoses .
|
-
- HY-N7628
-
Toralactone 9-O-β-D-gentiobioside
|
Endogenous Metabolite
|
Metabolic Disease
|
Cassiaside C (Toralactone 9-O-β-D-gentiobioside) is a naphthopyrone isolated from the seed of Cassia tora and has inhibitory activity on advanced glycation end products (AGE) formation in vitro .
|
-
- HY-144281
-
|
Bacterial
|
Infection
|
MsbA-IN-3 (compound 31) is a potent and highly selective MsbA inhibitor with an IC50 value of 2 nM. MsbA-IN-3 has inhibitory activity against Escherichia coli with a MIC of 35 μM .
|
-
- HY-144282
-
|
Bacterial
|
Infection
|
MsbA-IN-4 (compound 32) is a potent and highly selective MsbA inhibitor with an IC50 value of 3 nM. MsbA-IN-4 has inhibitory activity against Escherichia coli with a MIC of 12 μM .
|
-
- HY-147706
-
|
Others
|
Cancer
|
Ar524 has higher inhibitory activity than the known transgenic inhibitor kifunensine. At the same time, ar524 inhibited low concentration (10 μ M) Spheroid formation of human malignant cells.
|
-
- HY-152669
-
|
Bacterial
|
Infection
|
Urease-IN-5 is an inhibitor of urease with an IC50 value of 1.473 µM. Urease-IN-5 has low cytotoxicity and inhibitory activity on P. vulgaris with an IC50 value of 17.78 µg/mL .
|
-
- HY-N11637
-
|
HMG-CoA Reductase (HMGCR)
|
Inflammation/Immunology
|
Ganoderenic acid K is a natural product, that can be isolated from fruiting bodies of Ganoderma lucidum. Ganoderenic acid K shows strong inhibitory activity against HMG-CoA reductase (HMGCR) with IC50 of 16.5 μM .
|
-
- HY-P5286
-
|
Bacterial
|
Infection
Cancer
|
BMAP-27 is an antimicrobial peptide capable of disrupting the membrane integrity of microorganisms. Due to its membrane permeability, MAP-27 has inhibitory activity against both bacteria and cancer cells .
|
-
- HY-149239
-
|
Topoisomerase
HDAC
Apoptosis
|
Cancer
|
Topo II/HDAC-IN-2 (8d) exhibits excellent dual inhibitory activities against Topo II and HDAC. Topo II/HDAC-IN-2 (8d) induces apoptosis .
|
-
- HY-149238
-
|
Topoisomerase
HDAC
Apoptosis
|
Cancer
|
Topo II/HDAC-IN-1 (7d) exhibits excellent dual inhibitory activities against Topo II and HDAC. Topo II/HDAC-IN-1 (8d) induces apoptosis .
|
-
- HY-N2809
-
|
Others
|
Others
|
Acantrifoside E (Compound 8) is a nature compound. Acantrifoside E can be isolated from the 90% ethanol extract of Salacia cochinchinensis. Acantrifoside E has none α-glucosidase inhibitory activity .
|
-
- HY-N3211
-
cis-N-(4-Hydroxyphenethyl) ferulamide; cis-N-Feruloyltyramine
|
NO Synthase
|
Inflammation/Immunology
|
N-cis-Feruloyl tyramine (cis-N-(4-Hydroxyphenethyl) ferulamide) is a natural phenolic compound, exhibits modest inhibitory activity on LPS-activated NO production in RAW 264.7 cells .
|
-
- HY-N7324
-
|
COX
|
Inflammation/Immunology
|
Dehydroperilloxin is a natural compound isolated from the dichloromethane extract of the stems of Perilla frutescens var. acuta. Dehydroperilloxin possesses inhibitory activity against cyclooxygenase-1, with the IC50 value of 30.4 μM .
|
-
- HY-N8007
-
|
Others
|
Metabolic Disease
|
Quercetin 3-O-Glc-(1→2)-Rha-7-O-Rha is a flavonol glycoside with no significant inhibitory activity against albumin oleate-induced lipid accumulation.
|
-
- HY-N12637
-
|
Parasite
|
Infection
|
Kagimminol B, a cembrene-type diterpenoid, can be isolated from an Okeania sp. marine cyanobacterium. Kagimminol B shows selective growth-inhibitory activity against the causative agent of human African trypanosomiasis .
|
-
- HY-113614
-
|
Bacterial
|
Infection
|
Tetrahydrobostrycin is a secondary metabolite from Aspergillus sp., which exhibits a weak inhibitory activity against Staphylococcus aureus and Escherichia coli (100 mg/disc with the inhibition zones of 15 and 9.2 mm in diameter) .
|
-
- HY-N2621
-
|
Others
|
Inflammation/Immunology
|
Evodol is a natural product isolated from the dried and nearly ripe fruits of Euodia rutaecarpa. Evodol shows inhibitory activity against NO production . Evodol possesses larvicidal activity against the Asian tiger mosquitoes with a LC50 value of 32.43 μg/ml .
|
-
- HY-N7505
-
|
Bacterial
|
Infection
|
Norchelerythrine is an alkaloid isolated from the roots of Zanthoxylum capense with antibacterial activity against gram-positive and gram-negative bacteria. Norchelerythrine exhibits inhibitory activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Enterococcus faecalis and Escherichia coli with MIC values >50 µg/mL .
|
-
- HY-130079
-
Penicillin G procaine
|
Bacterial
|
Infection
|
Procaine benzylpenicillin (Penicillin G procaine) is an antimicrobial agent. Procaine benzylpenicillin shows inhibitory activity against gram-positive bacteria and synergistic activity with Neomycin (HY-B0470). Procaine benzylpenicillin can be used in the study of bovine mastitis in animal husbandry .
|
-
- HY-155702
-
|
Fungal
|
Infection
|
Antifungal agent 66 (compound 10) has antifungal activity. Antifungal agent 66 has a broad-spectrum antifungal activity against seven phytopathogenic fungal mycelia. Antifungal agent 66 has pronounced inhibitory activity against the spore of B. cinerea with an IC50 value of 47.7 μg/mL .
|
-
- HY-N1510
-
|
Glucosidase
|
Metabolic Disease
|
Kaempferol 3-O-gentiobioside is a flavonoid isolated from C. alata leaves with antidiabetic activity. Kaempferol 3-O-gentiobioside possesses activity against α-glucosidase and displays carbohydrate enzyme inhibitory effect with an IC50 of 50.0 µM .
|
-
- HY-N6891
-
|
COX
|
Inflammation/Immunology
|
Hamaudol is a chromone isolated from Saposhnikovia divaricata. Hamaudol shows significant inhibitory activity on cyclooxygenase (COX)-1 and COX-2 activities with IC50 values of 0.30, 0.57 mM, respectively, and has potent analgesia and anti-inflammary effects .
|
-
- HY-N0495
-
Aloenin A
|
Beta-secretase
|
Neurological Disease
|
Aloenin (Aloenin A) is a kind of natural product, has effective clearing and free radical activity, and has moderate inhibitory activity on β-secretion (BACE) (IC50=14.95 μg/mL). Aloenin suppresses peritoneal hypertrophy in large rats and suppresses its release.
|
-
- HY-19356A
-
|
Eukaryotic Initiation Factor (eIF)
Apoptosis
|
Cancer
|
Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. Didesmethylrocaglamide has potent growth-inhibitory activity with an IC50 of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity .
|
-
- HY-107703
-
|
iGluR
|
Neurological Disease
|
CGP 39551 is a potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonist with potent anticonvulsant activity . CGP 39551 shows measurable inhibitory activity at both L-[ 3H]-glutamate (Ki=8.4 μM) .
|
-
- HY-146195
-
-
- HY-119975
-
DC118
|
Reactive Oxygen Species
|
Cancer
|
Carazostatin (DC118), an antioxidant, can be isolated from Streptomycs chromofuscus. Carazostatin (DC118) exhibits strong inhibitory activity against free radical-induced lipid peroxidation and shows stronger antioxidant activity in liposomal membranes than α-tocopherol (VE) .
|
-
- HY-W009248
-
|
COX
Lipoxygenase
|
Inflammation/Immunology
|
Phenethyl ferulate is a major constituent ofQianghuo, shows inhibitory activity against cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) with IC50 values of 4.35 μM and 5.75 μM, respectively .
|
-
- HY-134598A
-
|
Epigenetic Reader Domain
|
Cancer
|
653-47 hydrochloride, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 hydrochloride is also a very weak CREB inhibitor with IC50 of 26.3 μM .
|
-
- HY-134598
-
|
Epigenetic Reader Domain
|
Cancer
|
653-47, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 is also a very weak CREB inhibitor with IC50 of 26.3 μM .
|
-
- HY-N5051
-
|
Others
|
Inflammation/Immunology
|
25(S)-Ruscogenin-1-O-α-L-rhamnopyranosyl (1→2)-β-D-xylopyranoside shows inhibitory activity of neutrophil respiratory burst stimulated by PMA(phorbol myristate acetate) .
|
-
- HY-N1162
-
Amentoflavanone
|
Xanthine Oxidase
|
Infection
Inflammation/Immunology
|
Tetrahydroamentoflavone (Amentoflavanone) is a potent xanthine oxidase (XO) inhibitor. Tetrahydroamentoflavone has inhibitory activity for XO with IC50 and Ki values of 92 nM and 0.982 μM, respectively. Tetrahydroamentoflavone can be used for the research of inflammatory disorders and gout .
|
-
- HY-N10340
-
Clauszoline I
|
Others
|
Cancer
|
Clausine E, is a alkaloid which can be isolated from Clausena excavata, is a inhibitor of fat mass and obesity-associated protein (FTO) demethylase. Clausine E shows inhibitory activities against proliferation of synoviocytes and cancer cells.
|
-
- HY-N11841
-
|
Glucosidase
|
Metabolic Disease
|
Mortatarin G (compound 3) is a prenylated flavonoid, that can be isolated from mulberry leaves. Mortatarin G exhibits good α-glucosidase inhibitory activity, with an IC50 of 20.4±1.4 μM .
|
-
- HY-N2703
-
|
Glucosidase
|
Metabolic Disease
|
6β-Hydroxyipolamiide can be isolated from the methanolic extract of S. jamaicensis leaves. 6β-Hydroxyipolamiide has α-glucosidase inhibitory activity with an IC50 of 539.17 μg/mL .
|
-
- HY-155410
-
|
Endogenous Metabolite
|
Metabolic Disease
|
HPSE1-IN-1 (compound 16) is a selective inhibitor of Heparanase-1 (HPSE1) with moderate inhibitory activity against exo-β-d-glucuronidase (GUSβ) and glucocerebrosidase (GBA) .
|
-
- HY-P10202
-
|
STAT
|
Cancer
|
5-FAM-GpYLPQTV-NH2 is a fluorescently labeled peptide and has STAT3 inhibitory activity. 5-FAM-GpYLPQTV-NH2 can be used in cancer research .
|
-
- HY-113053
-
-
- HY-163395
-
|
Parasite
|
Infection
|
3-Tosylimidazolidine-2,4-dione (compound 2C) is a hydantoins derivative, and exhibits inhibitory activity against the Pf3D7 strain, with an IC50 value of 3.97 nM .
|
-
- HY-162417
-
|
Others
|
Others
|
PPO-IN-12 (Compound E-Ic) an inhibitor for nicotiana tabacum protoporphyrinogen IX oxidase (NtPPO), with the Ki of 3 nM. Antibacterial agent 208 exhibits a board herbicide spectrum, with good inhibitory activity against broadleaf weeds .
|
-
- HY-104048
-
QC6352
4 Publications Verification
|
Histone Demethylase
|
Cancer
|
QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B) .
|
-
- HY-N3023
-
NSC 263475 hydrobromide
|
DNA/RNA Synthesis
|
Cancer
|
3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibits DNA polymerase activity in melanoma cells . 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitory activity in melanoma cell lines with varying degrees of tyrosinase activity .
|
-
- HY-162356
-
|
PD-1/PD-L1
|
Cancer
|
PD-L1-IN-4 (Compound X18) is an orally active PD-L1 inhibitor that exhibits remarkable inhibitory activity against the PD-1/PD-L1 interaction (IC50 = 1.3 nM) and enhances PD-L1 inhibitory effect on T cells (EC50 = 152.8 nM). PD-L1-IN-4 can be used for the research of cancer .
|
-
- HY-12136
-
-
- HY-N1098
-
|
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
|
Velutin is an aglycone extracted from Flammulina velutipes, with inhibitory activity against melanin biosynthesis. Velutin reduces osteoclast differentiation and down-regulates HIF-1α through the NF-κB pathway .
|
-
- HY-19936A
-
|
Bacterial
|
Infection
|
ACHN-975 TFA is a selective LpxC inhibitor and exhibits a subnanomolar LpxC inhibitory activity. ACHN-975 TFA is against a wide range of gram-negative bacterias with low MIC values (≤1 μg/mL) .
|
-
- HY-N1120
-
(+)-Triptoquinone B
|
Interleukin Related
|
Inflammation/Immunology
|
Triptoquinone B ((+)-Triptoquinone B), a sesquiterpene alkaloid, is an interleukin-1 inhibitor. Triptoquinone B shows potent inhibitory activities against interleukin 1α and β releases for human peripheral mononuclear cells .
|
-
- HY-N10292
-
|
Fungal
Endogenous Metabolite
|
Infection
|
Chaetosemin J, an antifungal metabolite, exhibits inhibitory activity against plant pathogenic fungi Botrytis cinerea, Alternaria solani, Magnaporthe oryzae, and Gibberella saubinettii, with MIC values ranging from 12.5-25 μM .
|
-
- HY-152668
-
|
Bacterial
|
Infection
|
Urease-IN-4 is an effective inhibitor of urease with an IC50 value of 1.64 µM. Urease-IN-4 has low cytotoxicity and shows inhibitory activity on P. vulgaris with an IC50 value of 15.27 µg/mL .
|
-
- HY-110253
-
HIV-1 inhibitor 18A
|
HIV
|
Infection
|
18A (HIV-1 inhibitor 18A) is a reversible broad-spectrum HIV-1 inhibitor. 18A exhibits broad inhibitory activity against multiple HIV-1 strains by blocking the function of Env .
|
-
- HY-P4874
-
|
Melanocortin Receptor
|
Metabolic Disease
|
ACTH (7-38) (human) is the 7-38 fragment of human ACTH (1-39). human ACTH (1-39), known as a corticotropin inhibitory peptide (CIP), is an antagonist of the ACTH receptor and has no any corticosteroid activity .
|
-
- HY-155092
-
|
DNA/RNA Synthesis
|
Others
|
DNA polymerase-IN-2 (Compd 3c), a coumarin derivative, exhibits inhibitory activity against Taq DNA polymerase with IC50 of 48.25 μM , which can be used in value-added disease research .
|
-
- HY-N11994
-
|
TNF Receptor
|
Inflammation/Immunology
|
Aloeresin G is a chromone glycoside that can be isolated from Aloe. Aloeresin G has a weak inhibitory effect on TNFα-induced NF-κB transcriptional activity, with an IC 50 value of 40.02 μM .
|
-
- HY-N12527
-
|
NF-κB
|
Others
|
Hyperelamine A (compound 5) is a polycyclic polyprenylated acylphloroglucinols (PPAPs). Hyperelamine A exhibits inhibitory activity against LPS-activated NO production in BV-2 cells via TLR-4/NF κB signaling .
|
-
- HY-161065
-
|
Bacterial
|
Infection
|
HKI12134085 (compound 3) is an orally available antibacterial nitrobenzothiazinone (BTZ) derivative with activity against Mycobacterium tuberculosis. HKI12134085 has in vivo inhibitory potency in a BALB/c mouse model of Mycobacterium tuberculosis infection .
|
-
- HY-N12723
-
|
Fungal
|
Infection
|
Talaroderxine D (compound 4) has biofilm inhibitory effect. Talaroderxine D shows antimicrobial activities against Bacillus subtilis and Staphylococcus aureus with MIC values of 2.1 and 8.3 μg/mL .
|
-
- HY-W357738
-
|
Bacterial
|
Infection
|
Urease-IN-14 (compound 15) is an urease inhibitor and antioxidant. Urease-IN-14 shows DPPH radical scavenging and urease inhibitory activities with IC50 values 151.7 μM and 41.6 μM, respectively .
|
-
- HY-N7272
-
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase .
|
-
- HY-N11771
-
|
Others
|
Others
|
Glyurallin B is a flavonoid, that can be isolated from licorice (Glycyrrhiza inflata and Glycyrrhiza uralensis). Glyurallin B shows ABTS + radical scavenging activity and the inhibitory activity on lipid peroxidation, with EC50 values of 11.9 ± 0.58 μM and 15.3 ± 1.26 μM, respectivley .
|
-
- HY-B0319
-
UK-20349
|
Fungal
Antibiotic
|
Infection
|
Tioconazole (UK-20349) is an antifungal imidazole derivative with broad spectrum activity. Tioconazole has inhibitory active aginst several dermatophytes and several yeasts with MIC50s <3.12 mg/L and <9 mg/L, respectively .
|
-
- HY-N1549
-
Naringenin 7-0-glucoside
|
Enterovirus
Phosphatase
|
Infection
Metabolic Disease
|
Prunin is a potent inhibitor of human enterovirus A71 (HEVA71). Prunin shows strong inhibitory activity against protein tyrosine phosphatase 1B (PTP1B), with an IC50 of 5.5 µM .
|
-
- HY-W011100
-
-
- HY-N8104
-
|
Others
|
Inflammation/Immunology
|
15a-Hydroxy-3,11,23-trioxo-lanost-8,20-dien-26-oic acid, a Lanostane triterpenoid, possesses NO production inhibitory activities of LPS-induced microglia .
|
-
- HY-143762
-
|
Influenza Virus
|
Infection
|
Cap-dependent endonuclease-IN-12 (EXP-35) is a potent Cap-dependent endonuclease inhibitor with low cytotoxicity. Cap-dependent endonuclease-IN-12 shows inhibitory activity against H1N1 .
|
-
- HY-126989
-
|
Arp2/3 Complex
|
Cancer
|
19-O-Acetylchaetoglobosin A, a cytochalasan alkaloid, is a fungal metabolite originally isolated from C. globosum that has actin polymerization inhibitory and cytotoxic activities. 19-O-Acetylchaetoglobosin A is cytotoxic to HeLa cervical cancer cells .
|
-
- HY-103691A
-
|
Autophagy
Apoptosis
|
Cancer
|
ARN5187 trihydrochloride is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 trihydrochloride shows lysosomotropic potency and cytotoxicity. ARN5187 trihydrochloride induces apoptosis .
|
-
- HY-103691
-
|
Autophagy
Apoptosis
|
Cancer
|
ARN5187 is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomotropic potency and cytotoxicity. ARN5187 induces apoptosis .
|
-
- HY-N8406
-
|
Bacterial
Antibiotic
|
Infection
|
Monomethylsulochrin is a potent antibacterial metabolite from endophytic fungus Aspergillus fumigatus, isolated from Albizia lucidior leaves (fabaceae). Monomethylsulochrin exhibits anti-Staphylococcus aureus activity with minimum inhibitory concentration (MIC) of 31.25 μg/mL .
|
-
- HY-120428
-
|
mGluR
|
Neurological Disease
|
VU0410425 is an mGlu1 negative allosteric modulator. VU0410425 exhibits potent inhibitory activity for rat mGlu1 with an IC50 value of 140 nM. VU0410425 can be used for the research of central nervous system disorders .
|
-
- HY-N8646
-
|
Others
|
Cancer
|
Isodonal is a N-pentane diterpene compound with potential cytotoxic, antitumor, inhibitory oxidative phosphorylation and antiingestion activities. Isodonal can be isolated from the leaves of Isodon wikstroemioides and is used in the study of gastrointestinal diseases, anti-tumor and anti-inflammatory .
|
-
- HY-155040
-
|
Biochemical Assay Reagents
|
Cancer
|
Antitumor agent-106 (compound 42) is an anticancer agent that exhibits good inhibitory activity (IC50=4.2-6.6 µM) against both lung cancer and colon cancer cell lines .
|
-
- HY-N10097
-
|
Na+/K+ ATPase
Bacterial
|
Infection
|
Chamigrenol is a Na +/K +-ATPase inhibitor with an IC50 value of 15.9 μg/mL. Chamigrenol shows strong inhibitory activities against Gram-positive and Gram-negative bacteria except Escherichia coli, with MIC values of 50 µg/mL .
|
-
- HY-N11892
-
|
NF-κB
|
Others
|
7-O-Methylaloesinol is a chromone derivative. 7-O-Methylaloesinol shows significant inhibitory effects against TNFα-induced NF-κB transcriptional activity with an IC50 value of 29.07 μM .
|
-
- HY-149516
-
|
Others
|
Others
|
Human enteropeptidase-IN-3 is an enteropeptidase inhibitor. Human enteropeptidase-IN-3 exhibits enteropeptidase activity and long duration of inhibitory state. Human enteropeptidase-IN-3 can be used for intetinal digestive related diseases research .
|
-
- HY-133850
-
|
Pim
|
Cancer
|
10-DEBC is a selective Akt inhibitor. 10-DEBC shows strong inhibitory activity against Moloney murine leukemia virus (Pim) kinase-1 (IC50=1.28 μM) .
|
-
- HY-W745164
-
|
MMP
|
Inflammation/Immunology
|
3,3′-Bisdemethylpinoresinol, lignin, is a nature product and has MMP-1 inhibitory activity in UVA-irradiated human dermal fibroblasts. 3,3′-Bisdemethylpinoresinol can be isolated from the seeds of Morinda citrifolia .
|
-
- HY-157318
-
|
SHP2
|
Cancer
|
PB17-026-01 is a potent SHP2 allosteric inhibitor and shows the highest inhibitory activity with an IC50 value of 38.9?nM. PB17-026-01 can be used for the research of tumor .
|
-
- HY-162358
-
|
Dihydrofolate reductase (DHFR)
Bacterial
|
Infection
|
DHFR-IN-17 (compound j9) is an oral active SaDHFR inhibitor with the IC50 of 0.97 nM. DHFR-IN-17 shows antibacterial activity against S. aureus with the minimum inhibitory concentration of 0.031 μg/mL .
|
-
- HY-P10202A
-
|
STAT
|
Cancer
|
5-FAM-GpYLPQTV-NH2 (TFA) is a fluorescently labeled peptide and has STAT3 inhibitory activity. 5-FAM-GpYLPQTV-NH2 (TFA) can be used in cancer research .
|
-
- HY-149057
-
|
Influenza Virus
|
Infection
|
NDV-IN-1 is an antiviral agent with high neuraminidase inhibitory activity. NDV-IN-1 exhibits in vitro inhibitory activity against Newcastle disease virus (NDV). NDV-IN-1 significantly inhibits NDV infection of Vero cells by preventing the release of virus particles from infected cells . Neuraminidase-IN-12 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-120824
-
|
COX
|
Inflammation/Immunology
|
Mofezolac, a non-steroidal anti-inflammatory drug (NSAID), is a selective, reversible and orally active COX-1 inhibitor with an IC50 of 1.44 nM. Mofezolac shows weak inhibitory activity on COX-2 (IC50 of 447 nM). Mofezolac can relieve pain and has anti-inflammatory activities .
|
-
- HY-115999
-
|
Carbonic Anhydrase
|
Cancer
|
Carbonic anhydrase inhibitor 12 is a potent CA II inhibitor, also has inhibitory activity in CA I (Kis of 1.72 and 271 nM in CA II and CA I, respectively). Carbonic anhydrase inhibitor 12 has potent anticancer activity against different cancer cell lines .
|
-
- HY-N1170
-
(2R)-Taxiphyllin
|
Tyrosinase
|
Others
|
Taxiphyllin (2R-Taxiphyllin) is a plant cyanogenic glycoside, which exhibits inhibitory activity for tyrosinase . Taxiphyllin exhibits cytotoxicity in BRL-3A cellls with an IC50 of 18.75 μm and antimicrobial activities against Staphylococcus aureus with an EC50 of 0.96 μM .
|
-
- HY-P5016
-
|
Antibiotic
Bacterial
Fungal
|
Infection
Cancer
|
CRAMP-18 (mouse) is an antibiotic peptide without hemolytic activity. CRAMP-18 (mouse) has good inhibitory activity against Gram-negative bacteria, such as S. typhimurium and P. aeruginosa. CRAMP-18 (mouse) has the potential to study antifungal, antibacterial and antitumor .
|
-
- HY-N0136S
-
(+)-Dihydroquercetin-d3; (+)-Taxifolin-d3
|
Isotope-Labeled Compounds
Autophagy
Tyrosinase
|
Inflammation/Immunology
|
Taxifolin-d3 is deuterium labeled Taxifolin. Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM[1]. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity[2].
|
-
- HY-146460
-
|
Reactive Oxygen Species
|
Infection
|
Antimicrobial agent-2 (compound V-a) is a broad-spectrum antimicrobial agent, possessing inhibitory activity against various Gram-positive and -negative bacteria. Antimicrobial agent-2 has excellent inhibitory effect on Methicillin-resistant Staphylococcus aureus (MRSA) with a MIC of 1 μg/mL. Antimicrobial agent-2 can effectively damage the membrane and lead to the leakage of protein, also can induce the generation of ROS. Antimicrobial agent-2 exhibits low toxicity, no obvious resistance and good bioavailability .
|
-
- HY-13672
-
-
- HY-132198
-
|
Histone Demethylase
|
Cancer
|
JMJD7-IN-1 is a potent JMJD7 inhibitor, with an IC50 of 6.62 μM. JMJD7-IN-1 shows good inhibitory activity against cells expressing a high level of JMJD7 .
|
-
- HY-N2658
-
|
Phosphodiesterase (PDE)
|
Others
|
5,7-Diacetoxy-8-methoxyflavone is a natural product that could come from scutellaria genus plants. 5,7-Diacetoxy-8-methoxyflavone has inhibitory activity for cAMP phosphodiesterase .
|
-
- HY-103237
-
|
Adenosine Deaminase
|
Neurological Disease
|
L-Adenosine is a metabolically stable enantiomeric analog and also is a potential probe. L-Adenosine has weakly inhibitory adenosine deaminase (ADA) activity with an Ki value of 385 μM. L-Adenosine can be used for the research of adenosine uptake and accumulation .
|
-
- HY-N10108
-
|
Xanthine Oxidase
|
Inflammation/Immunology
|
Protosappanin A dimethyl acetal is a homoisoflavonoid. Protosappanin A dimethyl acetal can be isolated from Caesalpinia sappan. Protosappanin A dimethyl acetal is also a competive inhibitor with significant xanthine oxidase inhibitory activity (IC50=50.7 μM) .
|
-
- HY-N8523
-
|
Others
|
Metabolic Disease
|
Vibralactone D (Compound 1) is a metabolite isolated and cultured from natural basidiomycetes Boreostereum vibrans. Vibralactone D shows weak inhibitory activity against isoenzymes of 11b-hydroxysteroid dehydrogenase (HSD) (IC50 85.7 μM).
|
-
- HY-149671
-
|
Others
|
Inflammation/Immunology
|
Anti-inflammatory agent 63 is an anti-inflammatory agent that shows optimal inhibitory activity (EC50 = 5.33±0.57 μM) against the production of nitric oxide (NO) induced by lipopolysaccharide (LPS) in RAW264.7 cells .
|
-
- HY-163182
-
|
Casein Kinase
|
Infection
|
CSNK2A-IN-2 (compound 6c) is a selective CSNK2A inhibitor with antiviral activity. CSNK2A-IN-2 exhibits an inhibitory effect on viral replication and is selective for PIM3 .
|
-
- HY-Y0790S
-
p-Isopropylbenzaldehyde-d8
|
Endogenous Metabolite
Isotope-Labeled Compounds
|
Cancer
|
Cuminaldehyde-d8 is deuterated labeled Cuminaldehyde (HY-Y0790). Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity .
|
-
- HY-W022047
-
-
- HY-157446
-
|
Fungal
|
Infection
|
MoTPS1/2-IN-1 (Compound A1-4 ) is a bispecific inhibitor of MoTps1 and MoTps2. MoTPS1/2-IN-1 has antifungal activity and showed good inhibitory activity against the growth and virulence of B. cinerea and F. graminearum .
|
-
- HY-N6252
-
|
Others
|
Cancer
|
Gypenoside XLVI is one of the major dammarane-type triterpenoid saponins from Gynostamma pentaphallum . Gypenoside XLVI has a tetracyclic triterpene structure and possess potent non-small cell lung carcinoma A549 cell inhibitory activity .
|
-
- HY-107523A
-
|
EAAT
|
Neurological Disease
|
WAY-213613 (hydrochloride) is a potent and selective human EAAT2 inhibitor. WAY-213613 has potent EAAT2 inhibitory activity with an IC50 value of 85 nM. WAY-213613 can be used for the research of central nervous system .
|
-
- HY-N2481
-
Oroxyloside; Oroxylin A-7-O-β-D-glucuronide
|
Prolyl Endopeptidase (PREP)
|
Neurological Disease
|
Oroxylin A-7-O-glucuronide (Oroxyloside; Oroxylin A-7-O-β-D-glucuronide) is a flavonoid glucuronide isolated from the dried root of Scutellaria baicalensis, with prolyl oligopeptidase (POP) inhibitory activity .
|
-
- HY-P1149
-
Epithalon; Epithalamin
|
Telomerase
|
Neurological Disease
Cancer
|
Epitalon is an anti-aging agent and a telomerase activator. Epitalon has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon can be used for cancer, old age and Retinitis Pigmentosa .
|
-
- HY-120438
-
|
PI3K
Akt
|
Inflammation/Immunology
|
TASP0415914 is a potent and orally active PI3Kγ inhibitor with an IC50 of 29 nM. TASP0415914 also shows potent Akt inhibitory activities with an IC50 of 294 nM. TASP0415914 can be used for inflammatory diseases research .
|
-
- HY-118463
-
|
Neurokinin Receptor
|
Neurological Disease
|
Benzomalvin A is a potent antagonist of neurokinin receptor isolated from Penicillium sp. Benzomalvin A shows inhibitory activity against substance P with Ki values of 12, 42 and 43 μM at the guinea pig, rat and human neurokinin NK1 receptors, respectively .
|
-
- HY-N10472
-
|
STAT
|
Cancer
|
STAT3-IN-14 (Compound 1) is a STAT3 inhibitor and has STAT3 phosphorylation inhibitory activity. STAT3-IN-14 (Compound 1) can directly bind to the hinge region of STAT3 .
|
-
- HY-147216A
-
|
Lactate Dehydrogenase
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
AXKO-0046 dihydrochloride, indole derivative, is an uncompetitive Lactate dehydrogenase B (LDHB) selective inhibitor. AXKO-0046 dihydrochloride has LDHB inhibitory activity with an EC50 value of 42 nM. AXKO-0046 dihydrochloride can be used for the research of cancer metabolism .
|
-
- HY-162086A
-
|
HDAC
|
Cancer
|
HDAC-IN-69 (Compound 29) has inhibitory activity against HDACs (IC50=0.04 μM) and fragments microtubules by activating katanin, a microtubule-severing protein. HDAC-IN-69 can be used in cancer research .
|
-
- HY-160196
-
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
GCN2 modulator-1 (compound 3) has GCN2 inhibitory activity, with the IC50 value less than 0.05 μM. GCN2 modulator-1 plays an important role in anti-tumor research .
|
-
- HY-N8329
-
|
Fungal
Antibiotic
|
Infection
|
AS-2077715 is an antifungal agent that shows inhibitory activity against the Trichophyton species. AS-2077715 can be obtained from the fermentation broth of Capnodium sp. 339855. AS-2077715 can be used to study fungal infections .
|
-
- HY-15517
-
|
Others
|
Cancer
|
KN-92 is an inactive derivative of KN-93, without CaM kinase inhibitory activity. KN-92 is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 is a cell-permeable, reversible and competitive CaMKII inhibitor .
|
-
- HY-15517A
-
|
Others
|
Cancer
|
KN-92 phosphate is an inactive derivative of KN-93, without CaM kinase inhibitory activity. KN-92 phosphate is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 is a cell-permeable, reversible and competitive CaMKII inhibitor .
|
-
- HY-N2443
-
|
Bacterial
|
Infection
Neurological Disease
|
Tribuloside is a flavonoid that can be isolated from Tribulus terrestris L . Tribuloside exhibits anti-mycobacterial activity against the non-pathogenic Mycobacterium species with a minimum inhibitory concentration (MIC) of 5.0 mg/mL. Tribuloside has 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity .
|
-
- HY-N11128
-
|
Kinesin
|
Cancer
|
Solidagonic acid inhibits HSET motor activity by promoting the conversion from abnormal monopolar to bipolar spindles. Solidagonic acid suppresses fission yeast cell death and enables reversion of the mitotic spindles from a monopolar to bipolar morphology. Solidagonic acid showed the growth inhibitory activity on the seedlings of Lactuca sativa L. and Lolium multiflorum Lam .
|
-
- HY-149846
-
|
EGFR
|
Cancer
|
SIQ17 is an EGFR inhibitor that inhibits its activity by occupying the ATP-binding site, with IC50 of 0.62 nM. SIQ17 shows more effective EGFR-TK inhibitory activity compared to the known inhibitor Erlotinib (HY-50896) (IC50 of ∼20 nM). SIQ17 can be used for cancer research
|
-
- HY-162388
-
|
AAK1
|
Neurological Disease
|
TIM-098a is a selective AAK1 inhibitor with an IC50 of 0.24 µM. TIM-098a has no inhibitory activity against CaMKK isoforms. TIM-098a inhibits AAK1-regulated endocytosis by suppressing AAK1 kinase activity .
|
-
- HY-125300
-
|
Fungal
Antibiotic
|
Cancer
|
Oligomycin E is a antitumor antibiotic that can be isolated from Streptomyces. Oligomycin E has significant antifungal activity, showing minimal inhibitory concentrations (MICs) values between 2 and 75μg/mL. Oligomycin E has strong antitumor activity against HeLa cells, with an IC50 of 0.014 μg/mL .
|
-
- HY-N3014
-
|
Notch
Apoptosis
Parasite
|
Infection
Cancer
|
Bruceine D is a Notch inhibitor with anti-cancer activity and induces apoptosis in several human cancer cells. Bruceine D is an effective botanical insect antifeedant with outstanding systemic properties, causing potent pest growth inhibitory activity . Bruceine D has strong anthelmintic activity against D. intermedius with an EC50 value of 0.57 mg/L .
|
-
- HY-13454
-
|
PKD
|
Cancer
|
CID 2011756 is an ATP competitive PKD inhibitor, with an IC50 of 3.2 µM for PKD1 in cell free assay, and also shows cellular pan-PKD inhibitory activity against PKD2 and PKD3 (IC50, 0.6 and 0.7 µM, respectively). CID 2011756 also has antitumor activity.
|
-
- HY-N2298
-
|
Apoptosis
|
Cancer
|
Camellianin A, the main flavonoid in A. nitida leaves, displays anticancer activity and angiotensin converting enzyme (ACE)-inhibitory activity. Camellianin A inhibits the proliferation of the human Hep G2 and MCF-7 cell lines and induces the significant increase of the G0/G1 cell population .
|
-
- HY-116999
-
|
HBV
|
Infection
|
IR415 is a potent anti-HBV agent and inhibits HBV replication by blocking the HBx activity. IR415 selectively interacts with HBx (Kd=2 nM) and blocks HBV-mediated RNAi suppression, reverses the inhibitory effect of HBx protein on the activity of the dicer endoribonuclease . HBx: hepatitis B virus X protein.
|
-
- HY-N7430
-
|
Bacterial
|
Infection
Inflammation/Immunology
|
3-O-Methylellagic acid is a nature product that can be isolated from Myrciaria cauliflora, with anti-inflammatory activity. 3-O-Methylellagic acid shows an inhibitory effect on glucose transport assay. 3-O-Methylellagic acid has antibacterial activity, with a MIC of 32 μg/mL for Staph. Aureus ATCC 25923 .
|
-
- HY-146699
-
|
Bacterial
Thymidylate Synthase
|
Infection
|
MtTMPK-IN-5 (compound 17) is a potent M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC50 value of 34 μM. MtTMPK-IN-5 combines favorable enzyme inhibitory activity with significant activity against M. tuberculosis (MIC = 12.5 μM). MtTMPK-IN-5 can be used for researching tuberculosis .
|
-
- HY-N9404
-
|
Sodium Channel
|
Neurological Disease
|
6-Benzoylheteratisine is an Aconitum alkaloid with potential neuroprotective activity. 6-Benzoylheteratisine can antagonize tetrodotoxin, inhibit the increase of [Na +]i, [Ca 2+]i and glutamate release, and block sodium channels. 6-Benzoylheteratisine has an inhibitory effect on the neuronal activity underlying epileptiform burst discharge .
|
-
- HY-N10755A
-
|
Cytochrome P450
Bacterial
|
Infection
|
(±)-ε-Viniferin is a racemate of ε-Viniferin (HY-N3841). (±)-ε-Viniferin exhibits P450 inhibitory antioxidants, as well as hepato-protective and antimicrobial activities. (±)-ε-Viniferin has antibacterial and antibiofilm activity against Gram-positive bacteria Streptococcus pneumoniae with a MIC of 20 μM .
|
-
- HY-10520
-
|
MNK
Apoptosis
|
Cancer
|
CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC50 of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.
|
-
- HY-107523
-
|
EAAT
|
Neurological Disease
|
WAY-213613 is a potent and selective human EAAT2 inhibitor. WAY-213613 has potent EAAT2 inhibitory activity with an IC50 value of 85 nM. WAY-213613 can be used for the research of central nervous system
|
-
- HY-N0223
-
-
- HY-137954
-
|
SARS-CoV
|
Infection
|
GRL-0496 is a potent chloropyridyl ester-derived SARS-CoV 3CLpro inhibitor, with an IC50 of 30 nM in both enzyme inhibitory and antiviral assays. GRL-0496 shows SARS-CoV antiviral activity, with an EC50 of 6.9 μM .
|
-
- HY-132914
-
|
CDK
|
Cancer
|
CDK/HDAC-IN-1 shows remarkable CDK2/4/6 and HDAC6 inhibitory activity of IC50 = 60.9 ± 2.9, 276 ± 22.3, 27.2 ± 4.2, and 128.6 ± 0.4 nM, respectively.
|
-
- HY-122675
-
|
Others
|
Cancer
|
ACG416B (compound 18) is a potent inhibitor of ChoK (choline kinase) with an IC50 of 0.4 μM. ACG416B renders higher ChoK inhibitory and antiproliferative activities against the HT-29 human colon cancer cell .
|
-
- HY-147216
-
|
Lactate Dehydrogenase
|
Cancer
|
AXKO-0046, indole derivative, is an uncompetitive Lactate dehydrogenase B (LDHB) selective inhibitor.AXKO-0046 has LDHB inhibitory activity with an EC50 value of 42 nM.AXKO-0046 can be used for the research of cancer metabolism .
|
-
- HY-W029411
-
|
Others
|
Cancer
|
4-(Benzo[d]oxazol-2-yl)aniline is a potent antitumor agent. 4-(Benzo[d]oxazol-2-yl)aniline has inhibitory activity against mammary carcinoma cell lines .
|
-
- HY-113632
-
10Z-Debromohymenialdisine
|
Raf
MEK
|
Cancer
|
Debromohymenialdisine (10Z-Debromohymenialdisine) is a pyrrole alkaloid. Debromohymenialdisine has moderate inhibitory activity with an IC50 value of 881 nM in the initial Raf/MEK-1/MAPK signaling cascade assay. Debromohymenialdisine can be used for the research of proliferation and differentiation .
|
-
- HY-151974
-
|
Xanthine Oxidase
|
Metabolic Disease
|
Xanthine oxidoreductase-IN-4 is an orally active xanthine oxidoreductase (XOR) inhibitor. Xanthine oxidoreductase-IN-4 has inhibitory activity against XOR with an IC50 value of 29.3 nM. Xanthine oxidoreductase-IN-4 can be used for the research of hyperuricemia .
|
-
- HY-18309
-
|
c-Met/HGFR
VEGFR
|
Cancer
|
MET kinase-IN-4 is an orally active Met kinase inhibitor. MET kinase-IN-4 has potent Met kinase inhibitory activity with an IC50 value of 1.9 nM. MET kinase-IN-4 can be used for the research of cancer .
|
-
- HY-120577
-
|
Others
|
Cardiovascular Disease
|
BA 41899 is a purely calcium-sensitizing agent. BA 41899 is completely devoid of phosphodiesterase (PDE) III inhibitory activity or any other known inotropic mechanism. BA 41899 can be used for the research of cardiovascular diseases, such as congestive heart failure (CHF) .
|
-
- HY-153329
-
|
TNF Receptor
|
Others
|
TNF-α-IN-9 (compound 48) is a analog of NDM-1 inhibitor-3 (HY-150758). TNF-α-IN-9 is a TNF-α inhibitor. TNF-α-IN-9 shows low inhibitory activity .
|
-
- HY-N2906
-
Atalantoflavone
|
Parasite
|
Cancer
|
Limonianin (Atalantoflavone) is a flavone, that can be isolated from Erythrina sigmoidea and the root bark of Citrus limonia. Limonianin presents inhibitory effect against P. gingivalis. Limonianin shows cytotoxic activity against multidrug-resistant (MDR) cancer cell lines .
|
-
- HY-155136
-
|
SARS-CoV
|
Infection
|
NSC89641 inhibits MERS-CoV M pro, with an IC50 value < 3.5 μM. NSC89641 exhibits the high inhibitory potency against SARS-CoV-2 M pro enzymatic activity, with an IC50 of 3.05 μM .
|
-
- HY-N12200
-
|
Others
|
Cancer
|
Mollicellin I (compound 1) is a depsidone. The growth inhibitory activity of Mollicellin I on human breast cancer (Bre04), human lung (Lu04) and human neuroma (N04) cell lines is not significant, with GI50s >10 μg/mL .
|
-
- HY-156778
-
|
Others
|
Cancer
|
Antitumor agent-120 (compound 1) is a flavonoid compound isolated from Kudzu root.Antitumor agent-120 has no significant inhibitory activity against LNCaP and PC3 cancer cells, with IC50s >50 μM .
|
-
- HY-N12347
-
|
Others
|
Inflammation/Immunology
|
α-Glucosidase-IN-37 (Compound 11) moderately inhibits LPS-induced NO production with an IC50 value of 23.7 μM in macrophages. α-Glucosidase-IN-37 has weak inhibitory activity against α-Glucosidase .
|
-
- HY-163104
-
|
Bacterial
|
Infection
|
Antibacterial agent 169 (Compound 28) is a pyrrolamide-type GyrB/ParE inhibitor with antibacterial activity. Antibacterial agent 169 has an inhibitory effect on Gyrase and Topo IV of Staphylococcus aureus, with IC50 values of 49 nmol/L and 1.513 μmol/L respectively .
|
-
- HY-162134
-
|
Parasite
|
Infection
|
Trypanothione synthetase-IN-5 (compound 9) is a trypanothione reductase (TR) inhibitor, with an IC50 of 20.5 μM for Leishmania infantum TR. Trypanothione synthetase-IN-5 also has inhibitory activity for human glutathione reductase (hGR), with an IC50 of 62.4 μM .
|
-
- HY-126462
-
|
Others
|
Infection
|
Lantic acid is a triterpenoid compound possessing antimicrobial activity. Lantic acid exhibits inhibitory effects on a broad range of both Gram-positive and Gram-negative bacteria, with particular potency against Escherichia coli and Bacillus subtilis. Lantic acid is utilized in the research and development of antimicrobial agents .
|
-
- HY-157527
-
|
Cholinesterase (ChE)
Beta-secretase
|
Neurological Disease
|
hAChE-IN-7 (compound 5s) is a mixed inhibitor affecting both the catalytic active site (CAS) and peripheral anionic site (PAS) of hAChE. hAChE-IN-7 displays the balanced inhibitory effect on hAChE (IC50=69.8 nM) and hBuChE (IC50=68.0 nM), and exhibits inhibitory activity against β-secretase-1 (BACE-1) (IC50=3.6 μM). hAChE-IN-7 has the potential for Alzheimer's disease (AD) research .
|
-
- HY-107412
-
PS-IX; AM114
|
Proteasome
|
Cancer
|
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53 +/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity .
|
-
- HY-N2795
-
Xanthone I
|
Parasite
Bacterial
|
Infection
|
9-Hydroxycalabaxanthone (Xanthone I) is a known xanthone isolated from Garcinia mangostana Linn. 9-Hydroxycalabaxanthone has quorum-sensing inhibitory, anti-microbial, and anti-malarial activities (IC50=1.2-1.5 µM) .
|
-
- HY-N7623
-
|
Others
|
Cancer
|
Ursonic acid methyl ester is an esterified derivative of Ursolic acid (HY-N0140). Ursonic acid methyl ester shows growth inhibitory activity against four tumor cell lines, HL-60, BGC, Bel-7402 and Hela with ED50 values of >100 µg/ml .
|
-
- HY-139908
-
|
SARS-CoV
|
Infection
|
MERS-CoV-IN-1 exhibits excellent inhibitory activity against coronavirus. MERS-CoV-IN-1 is useful as a pharmaceutical composition for preventing coronavirus-induced diseases (MERS-CoV and SARS) (extracted from patent WO2018174442A1, compound 1) .
|
-
- HY-151152
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
AChE-IN-24 is a potent AChE inhibitor and can penetrate the BBB. AChE-IN-24 has the mighty inhibitory activity to hAChE with an IC50 value of 0.053 μM. AChE-IN-24 can be used for the research of Alzheimer s disease (AD) .
|
-
- HY-Q40175
-
|
Parasite
|
Infection
|
Antitrypanosomal agent 9 (compound 1) is a potent antitrypanosomal agent. Antitrypanosomal agent 9 shows inhibitory activity against T. b. brucei, with an IC50 of 1.15 μM. Antitrypanosomal agent 9 can be used for human African trypanosomiasis (HAT) research .
|
-
- HY-N3185
-
|
Cholinesterase (ChE)
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
N-Methylcalycinine is a nature product with AChE inhibitory activity. N-Methylcalycinine can be isolated from the roots of Stephania epigaea. N-Methylcalycinine can be used for the research of asthma, cancer, dysentery, fever, hyperglycemia, intestinal complaints, inflammation, sleep disturbances, tuberculosis and so on .
|
-
- HY-149722
-
|
Parasite
|
Infection
|
Antiparasitic agent-20 (Compound 1p) is a parasite inhibitor with broad antiparasitic activity. Antiparasitic agent-20 has inhibitory effects on T. brucei and T. cruzi with EC50 values of 0.09 μM and 14.1 μM respectively .
|
-
- HY-N12507
-
|
STING
NF-κB
|
Others
|
Eupenicisirenin C (compound 1) is a sirenin derivative. Eupenicisirenin C has strong NF-κB inhibitory activities. Eupenicisirenin C suppresses effects on cGAS-STING pathway. Eupenicisirenin C inhibits RANKL-induced osteoclast differentiation in bone marrow macrophage cells .
|
-
- HY-N1186
-
|
Glucosidase
|
Metabolic Disease
|
Tachioside inhibits nitric oxide production in lipopolysaccharide (HY-D1056)-stimulated RAW 264.7 cells with IC50 value of 12.14 μM. Tachioside has anti-obesity, antioxidant and α-glucosidase inhibitory activities .
|
-
- HY-100659S
-
PCI-45227-d5
|
Btk
Isotope-Labeled Compounds
|
Cancer
|
Dihydrodiol-Ibrutinib-d5 is the deuterium labeled Dihydrodiol-Ibrutinib (HY-100659). Dihydrodiol-Ibrutinib is a dihydrodiol active metabolite of Ibrutinib (HY-10997), has inhibitory activity towards BTK approximately 15 times lower than that of ibrutinib .
|
-
- HY-W015307S
-
|
Biochemical Assay Reagents
Isotope-Labeled Compounds
|
Others
|
4-Ethyloctanoic acid- 13C2 is 13C labeled Cuminaldehyde (HY-Y0790). Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity .
|
-
- HY-158332
-
SKF-95587; BM-13177
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
Sulotroban (SKF-95587; BM-13177) is a selective antagonist for thromboxane A2 receptor (TXA2 Receptor). Sulotroban exhibits inhibitory activity against carbocyclic thromboxane A2- and endoperoxide-induced vasoconstrictor. Sulotroban inhibits platelets aggregation .
|
-
- HY-160873
-
|
Fluorescent Dye
|
Others
|
Firefly luciferase-IN-5 (CID: 16031203) is an inhibitor of ATP-dependent luciferase (Firefly luciferase). It has nM-level inhibitory activity against GRLuc, RLuc8, and RLuc respectively (pIC50=8.5,7.5,5.5) .
|
-
- HY-144123
-
|
HIV
|
Infection
|
HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1 inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitory activity or acute toxicity .
|
-
- HY-151364
-
|
HDAC
|
Cancer
|
HDAC6/8/BRPF1-IN-1 is a dual inhibitor of both HDAC6/8 and the bromodomain and PHD finger containing protein 1 (BRPF1). HDAC6/8/BRPF1-IN-1 has inhibitory activity for HDAC1, HDAC6 and HDAC8 with IC50 values of 797 nM, 344 nM and 908 nM, respectively. HDAC6/8/BRPF1-IN-1 has inhibitory activity for BRPF1 with an Kd value of 175.2 nM. HDAC6/8/BRPF1-IN-1 can be used for the research of cancer .
|
-
- HY-147919
-
|
Fungal
|
Infection
|
Antifungal agent 33 (compound 4e) is a potent antifungal agent. Antifungal agent 33 exhibits remarkable antifungal activity against C. albicans, with a MIC of 16 μg/mL. Antifungal agent 33 shows potent inhibitory activity against Lanosterol 14α-demethylase (CYP51), with an IC50 of 0.19 μg/mL .
|
-
- HY-151421
-
|
Fungal
|
Infection
Cancer
|
Chitin synthase inhibitor 11 is a chitin synthase inhibitor. Chitin synthase inhibitor 11 shows excellent chitin synthase inhibitory activity with an IC50 value of 0.10 mM. Chitin synthase inhibitor 11 has broad-spectrum antifungal activity in vitro. Chitin synthase inhibitor 11 can be used for the research of invasive fungal infections (IFIs) .
|
-
- HY-116940
-
|
Others
|
Cancer
|
Sm4 is a SOX18 inhibitor. Sm4 shows SOX18-DNA binding inhibitory activity. Sm4 selectively affects SOX18 transcriptional output in vitro. Sm4 blocks SoxF transcriptional activity in vivo. Sm4 can be used for cancer metastasis and vascular cancers research .
|
-
- HY-122664
-
|
BRK
|
Cancer
|
XMU-MP-2 is a BRK inhibitor with significant inhibitory activity on BRK-positive cells. XMU-MP-2 inhibits oncogenic BRK-driven tumor growth in a mouse xenograft model. XMU-MP-2 also synergizes with HER2 inhibitors or endoplasmic reticulum (ER) blockade to exert antiproliferative activity .
|
-
- HY-N0501
-
|
Reactive Oxygen Species
|
Metabolic Disease
|
11-oxo-mogroside V is a natural sweetener that exhibits strong antioxidant activity. It exhibits significant inhibitory effects on reactive oxygen species (O2 -, H2O2 and *OH) with EC50 of 4.79, 16.52, and 146.17 μg/mL, respectively.
|
-
- HY-112693
-
|
STING
|
Inflammation/Immunology
|
H-151 is a potent, selective and covalent antagonist of STING that has noteworthy inhibitory activity both in cells and in vivo. H-151 reduces TBK1 phosphorylation and suppresses STING palmitoylation. H-151 can be used for the research of autoinflammatory disease .
|
-
- HY-N2472
-
Castanogenin
|
Bacterial
|
Infection
|
Medicagenic acid (Castanogenin) is isolated from the roots of Herniaria glabra, exhibits potent fungistatic effects against several plant pathogens and human dermatophytes . Medicagenic acid (Castanogenin) has low enzyme inhibitory activities, the target enzymes are xanthine oxidase, collagenase, elastase, tyrosinase, ChE .
|
-
- HY-P1149A
-
Epithalon TFA; Epithalamin TFA
|
Telomerase
|
Neurological Disease
Cancer
|
Epitalon TFA is an anti-aging agent and a telomerase activator. Epitalon TFA has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon TFA can be used for cancer, old age and Retinitis Pigmentosa .
|
-
- HY-136063
-
|
Fungal
Cytochrome P450
|
Infection
|
Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent. Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM) .
|
-
- HY-N8167
-
Kaempferol 3-O-rhamnosylgentiobioside
|
COX
|
Inflammation/Immunology
|
Plantanone B is a moderate antioxidant-agent with an IC50 of 169.8±5.2 μM. Plantanone B shows significant ovine COX-1 and moderate COX-2 inhibitory activities. Plantanone B has the potential for inflammation-related diseases research .
|
-
- HY-135265
-
Ro 12-5637
|
Monoamine Oxidase
|
Neurological Disease
|
Moclobemide N-Oxide (Ro 12-5637) is N-oxide metabolite of Moclobemide. Moclobemide N-Oxide retains certain MAO-A (monoamine oxidase) inhibitory activity, but is generally present in low concentrations. Moclobemide N-Oxide can be detected by UV absorption at 240 nm .
|
-
- HY-147525
-
|
PROTACs
Histone Methyltransferase
|
Cancer
|
PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes .
|
-
- HY-139170
-
|
ROCK
|
Metabolic Disease
|
CAY10746 is a selective Rho kinase (ROCK) inhibitor. CAY10746 has inhibitory activity for ROCK I, ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. CAY10746 can be used for the research of diabetic retinopathy (DR) .
|
-
- HY-107055
-
|
Dopamine Transporter
|
Neurological Disease
|
RTI 336 is a phenyltropane analog, as well as a potent and selective dopamine transporter (DAT) inhibitor. RTI 336 inhibits addictive agent induced locomotor activity and self-administration in Lewis rats. RTI 336 exhibits inhibitory effects depending on inherent NAc DAT levels .
|
-
- HY-N12070
-
|
Others
|
Cardiovascular Disease
|
11-O-β-D-glucopyranosyl thamnosmonin, a coumarin glucosides, can be isolated from the roots of Angelica apaensis. 11-O-β-D-glucopyranosyl thamnosmonin has weak inhibitory activity on the aggregation of rabbit platelets induced by PAF, AA, and ADP .
|
-
- HY-113269
-
|
Others
|
Others
|
alpha-CEHC is a water-soluble metabolite of alpha-tocopherol (α-TOH) with potential antioxidant activity. alpha-CEHC slightly inhibits macrophage-induced low-density lipoprotein (LDL) oxidation, and its inhibitory potency is concentration-dependent .
|
-
- HY-161295
-
|
Carbonic Anhydrase
|
Cancer
|
hCAIX/XII-IN-10 (compound DK-8) is a carbonic anhydrase inhibitor. hCAIX/XII-IN-10 has potent inhibitory activity against tumor-associated membrane-bound isoforms hCA IX and XII, with Ki values of 32.5 nM and 29.2 nM .
|
-
- HY-162461
-
|
Reverse Transcriptase
HIV
|
Infection
|
HIV-1 inhibitor-66 is an orally active non-nucleoside reverse transcription inhibitor (NNRTI). HIV-1 inhibitor-66 shows inhibitory activity against wild-type HIV-1 reverse transcriptase with an IC50 of 40 nM .
|
-
- HY-101679
-
|
mAChR
|
Neurological Disease
|
YM-58790 is a potent antagonist of mAChR. YM-58790 binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats .
|
-
- HY-N7072
-
|
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
Grape seed extract is a natural product, with anti-inflammatory and anti-proliferative effects. Grape seed extract shows inhibitory activity on the fat-metabolizing enzymes pancreatic lipase and lipoprotein lipase. Grape seed extract induces apoptotic in human colorectal cancer cells .
|
-
- HY-144337
-
|
DNA Alkylator/Crosslinker
|
Cancer
|
DNA crosslinker 4 (dihydrochloride) is a potent DNA minor groove binder. DNA crosslinker 4 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 4 (dihydrochloride) can be used for researching anticancer .
|
-
- HY-N10407
-
|
Others
|
Metabolic Disease
|
Quercetin 3-O-rutinoside-7-O-glucoside (compound 8) is an antioxidant agent that canbe found in Hemerocallis fulva. Quercetin 3-O-rutinoside-7-O-glucoside shows strong lipid peroxidation inhibitory activities .
|
-
- HY-137823
-
|
Endogenous Metabolite
|
Cancer
|
4-Nitrophenyl-N-acetyl-β-D-galactosaminide has inhibitory activity against GlcNAc and GalNAc with Kis of 1.15 mM and 0.51 mM, respectively. 4-Nitrophenyl-N-acetyl-β-D-galactosaminide is extracted from Trichomonas foetus (T. foetus)
|
-
- HY-151348
-
|
Beta-secretase
|
Neurological Disease
|
BACE1-IN-11 is a BACE1 inhibitor. BACE1-IN-11 has the BACE1 inhibitory activity with an IC50 value of 72 μM. BACE1-IN-11 can be used for the research of Alzheimer’s disease (AD) .
|
-
- HY-N8850
-
|
Others
|
Cancer
|
Angelol G, a coumarin, can be isolated from Campylotropis hirtella. Angelol G shows inhibitory activity for prostate specific antigen (PSA)IC50 value of 152.1μM. Angelol G can be used for the research of benign prostate hyperplasia (BPH) .
|
-
- HY-N2902
-
|
Others
|
Cancer
|
Artocarpin is an isoprenoid-substituted flavonoid, that can be isolated from the wood of Artocarpus heterophyllus. Artocarpin inhibits melanin biosynthesis in B16 melanoma cells without inhibiting tyrosinase. The presence of the isoprenoid-substituted moiety enhanced the inhibitory activity on melanin production in B16 melanoma cells .
|
-
- HY-155304
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
BuChE-IN-8 (compound 19c) is a butyrylcholinesterase (BuChE) inhibitor with an IC50 of 559 nM. BuChE-IN-8 possesses human β-secretase (BACE1) and Aβ40 aggregation inhibitory activities. BuChE-IN-8 has significant antiamnesic properties .
|
-
- HY-B0673S
-
AMR69-d5
|
TGF-beta/Smad
CCR
|
Inflammation/Immunology
Cancer
|
Pirfenidone-d5 is a deuterium labeled Pirfenidone. Pirfenidone is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities[1][2][3].
|
-
- HY-132174
-
|
Flavivirus
Dengue virus
Dihydroorotate Dehydrogenase
|
Infection
|
CHIKV-IN-2 is a potent inhibitor against Chikungunya virus (CHIKV), with excellent cellular antiviral activity (EC90=270 nM) and improved liver microsomal stability. CHIKV-IN-2 shows inhibitory activity against a cellular target Dihydroorotate Dehydrogenase (DHODH), which interacts with various viruses and regulate their replication via depleting intracellular pyrimidine pools .
|
-
- HY-155704
-
|
Others
|
Others
|
DPP-IV-IN-5 is isolated from the fruits of Lycium barbarum. DPP-IV-IN-5 exerts moderate agonistic activities for peroxisome proliferator-activated receptor (PPARγ) with EC50 values of 10.09 - 44.26 μM and also presents inhibitory activity on dipeptidyl peptidase-4 (DPPIV) with an IC50 value of 47.13 μM .
|
-
- HY-157138
-
|
Others
|
Cancer
|
MMP-9-IN-8 (Compound 3) is an MMP-9 inhibitor with inhibitory activities of 42.16% and 58.28% at 10 μM and 50 μM concentrations, respectively. MMP-9-IN-8 has anti-cancer activity and can induce apoptosis in MCF-7 cells with an IC50 value of 23.42 μM .
|
-
- HY-161357
-
|
PI4K
|
Infection
|
KR-27370 (compound 7f) is an antiviral agent and selective PI4KIIIβ/PI4KIIIα inhibitor (IC50: 3.1 nM/15.8 nM), against hRV, Ke Saatchivirus and other enteroviruses have inhibitory activity[1].br/ .
|
-
- HY-161472
-
|
Aldose Reductase
|
Cancer
|
Aldose reductase-IN-7 (Compound 6k) targets Aldose reductase. Aldose reductase-IN-7 exhibits potent enzyme inhibitory activity (Ki = 0.186 ± 0.020 μM), showing superiority to Epalrestat (HY-66009), which is currently in clinical use. Aldose reductase-IN-7 is less cytotoxic and possesses potent anticancer activity .
|
-
- HY-18621A
-
|
TOPK
Apoptosis
|
Cancer
|
OTS514 hydrochloride is a highly potent TOPK inhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positive cancer cells . OTS514 hydrochloride induces cell cycle arrest and apoptosis .
|
-
- HY-N6797
-
|
Bacterial
c-Met/HGFR
Antibiotic
|
Infection
Cancer
|
Meleagrin is a roquefortine C-derived alkaloid produced by fungi of the genus Penicillium and has antimicrobial and anti-proliferative activities. Meleagrin is a class of FabI inhibitor. Meleagrin is a lead c-Met inhibitory entity useful for the control of c-Met-dependent metastatic and invasive breast malignancies .
|
-
- HY-146036
-
|
Endogenous Metabolite
|
Metabolic Disease
|
NADH-IN-1 has NADH:ubiquinone oxidoreductase inhibitory activity with an IC50 value of 27 μM. NADH-IN-1 can effectively stimulate glucose uptake in vitro. NADH-IN-1 is readily metabolised by the liver. NADH-IN-1 can be used for researching diabetes .
|
-
- HY-150697
-
|
HIV
|
Others
|
HIV-1 inhibitor-44 (compound 11l) is a HIV-1 reverse transcriptase inhibitor. HIV-1 inhibitor-44 shows inhibitory activity against wild-type HIV-1 strain with an EC50 value of 0.209 μM .
|
-
- HY-148489
-
|
Others
|
Cancer
|
CSNK1-IN-1 is a CSNK1A1 inhibitor. CSNK1-IN-1 has inhibitory activity for CSNK1A1 kinase with IC50 values of 21 μM. CSNK1-IN-1 can be used for the research of proliferative disorders .
|
-
- HY-P4095
-
|
CXCR
|
Cancer
|
NoxaBH3 is a cysteine-based cross-linked peptide with increased cell permeability and higher inhibitory activity against Mcl-1. NoxaBH3 binds to the endogenous CXCR4 ligand to produce ubiquitin-Noxabh3 conjugate. NoxaBH3 is then delivered to cancer cells .
|
-
- HY-153590
-
|
PARP
|
Cancer
|
PARP-1-IN-4 is a PARP-1 inhibitor. PARP-1-IN-4 has inhibitory activity against PARP-1 with IC50 value of 302 μM. PARP-1-IN-4 can be used for the research of lung adenocarcinoma .
|
-
- HY-W195984
-
|
Others
|
Cancer
|
Z57346765 is a PGK1-specific inhibitor that reduces the activity of metabolic enzymes in PGK1 glycolysis and inhibits PGK1-dependent cell proliferation. Z57346765 exerts inhibitory effects against clear cell renal cell carcinoma (KIRC) .
|
-
- HY-12155
-
|
Sodium Channel
Calcium Channel
|
Neurological Disease
|
JNJ-26990990 is a broad-spectrum antiepileptic agent with oral activity. JNJ-26990990 can inhibit voltage-gated Na + channels and N-type Ca 2+ channels, but has a very weak inhibitory effect on human carbonic anhydrase-II (IC50 = 110 μM) .
|
-
- HY-17602
-
BBI503
|
Others
|
Cancer
|
Amcasertib (BBI503) is an orally active and small-molecule multi-kinase inhibitor. Amcasertib exhibits inhibitory activity against the NANOG and CD133 expression and cell viability in PC-9/GR cells. As an orally available cancer cell stemness kinase inhibitor with potential antineoplastic activity, it is currently being studied in phase I clinical trials in a number of cancers.
|
-
- HY-105416
-
UCN-1028C
|
Antibiotic
PKC
Apoptosis
|
Infection
Cancer
|
Calphostin C is a potent and specific inhibitor of protein kinase C. Calphostin C is an antitumor antibiotic. Calphostin C has 1000 times more inhibitory to protein kinase C with an IC50 of 0.05 μM than other protein kinases. Calphostin C induces apoptosis in some tumor cell lines. Calphostin C has potent cytotoxic activity and antitumor activity .
|
-
- HY-150045
-
|
Topoisomerase
Bacterial
|
Infection
|
TP0480066 is a selective topoisomerase II inhibitor with IC50s of 1.10 and 62.89 nM for DNA gyrase and topo IV, respectively. TP0480066 shows good activity of againsting various bacterial species including drug-resistant strains. TP0480066 also exhibits potent inhibitory activity to N. gonorrhoeae, can be used in study of gonorrhea .
|
-
- HY-N9051
-
|
Glucosidase
|
Inflammation/Immunology
Cancer
|
6-Prenylquercetin-3-Me ether is a natural product that can be extracted from G. uralensis leaves.
6-Prenylquercetin-3-Me ether has radical scavenging activity toward DPPH. 6-Prenylquercetin-3-Me ether also has inhibitory activity against α-glucosidase .
|
-
- HY-155135
-
|
HPPD
|
Others
|
HPPD-IN-1 (compound II-3) is a HPPD inhibitor. HPPD-IN-1 shows inhibitory activity of Arabidopsis thaliana HPPD (AtHPPD) with an IC50 value of 0.248 μM, which was superior to that of mesotrione (HY-12853) (0.283 μM) in vitro. HPPD-IN-1 shows excellent herbicidal activity against broadleaf and monocotyledonous weeds .
|
-
- HY-N1839
-
|
Apoptosis
Glucosidase
|
Cancer
|
3-Hydroxybakuchiol can be isolated from Otholobium mexicanum J. W. Grimes. 3-Hydroxybakuchiol is an electron transport chain (ETC) inhibitor. 3-Hydroxybakuchiol has antitumor activity, and induces tumor cell apoptosis. 3-Hydroxybakuchiol also has moderate inhibitory activity against α-glucosidase (IC50: 345 μM) .
|
-
- HY-157044
-
|
Bacterial
|
Infection
Cancer
|
Antibacterial agent 162 trifluoromethanesulfonate (compound 7) is an antibacterial agent that exhibits potent inhibitory activity against Staphylococcus aureus, including MRSA. Antibacterial agent 162 trifluoromethanesulfonate is also an anticancer agent and exhibits antiproliferative activity against colon cancer and non-small cell lung cancer cells. Antibacterial agent 162 trifluoromethanesulfonate can be used in anticancer and antibacterial research .
|
-
- HY-B1080
-
|
HIF/HIF Prolyl-Hydroxylase
Influenza Virus
|
Infection
Neurological Disease
|
Tilorone dihydrochloride is an orally active interferon (IFN) inducer with broad-spectrum antiviral activities. Tilorone dihydrochloride possesses robust anti-Severe fever with thrombocytopenia syndrome virus (SFTSV) activity in vitro and in vivo through stimulation of host innate immunity. Tilorone dihydrochloride can penetrate the blood-brain barrier to activate HIF in the CNS .Tilorone dihydrochloride exhibits an inhibitory activity with EC50 of 230 nM against Ebola virus (EBOV) .
|
-
- HY-N6972
-
|
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
|
-
- HY-111449
-
AHR antagonist 1
|
Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
Cancer
|
BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist. BAY-218 has AHR inhibitory activity with an IC50 of 39.9 nM in in U87 glioblastoma cells. BAY-218 can be used for the research of cancer or conditions with dysregulated immune responses .
|
-
- HY-N0577
-
|
NO Synthase
|
Inflammation/Immunology
|
Apiin, a major constituent of Apium graveolens leaves with anti-inflammatory properties. Apiin shows significant inhibitory activity on nitrite (NO) production (IC50 = 0.08 mg/mL) in-vitro and iNOS expression (IC50 = 0.049 mg/ mL) in LPS-activated J774.A1 cells .
|
-
- HY-N1416
-
|
Bacterial
Apoptosis
Autophagy
|
Infection
Inflammation/Immunology
|
Pogostone is isolated from patchouli oil with anti-bacterial and anti-cancer activities. Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 µg/ml . Pogostone induces cell apoptosis and autophagy .
|
-
- HY-P9921
-
Ado-Trastuzumab emtansine; PRO132365; T-DM 1
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine). Trastuzumab emtansine can be used for the research of advanced breast cancer .
|
-
- HY-124366
-
|
Others
|
Infection
Cancer
|
Slingshot inhibitor D3 is a potent, selective, reversible and competitive inhibitor of Slingshot. The IC50 value for Slingshot 1 is 3 μM and the Ki value for Slingshot 2 is 3.9 μM. Slingshot inhibitor D3 has similar inhibitory activities toward both Slingshot 1 and Slingshot 2 .
|
-
- HY-111934
-
|
Parasite
|
Others
Cancer
|
Cymarin, a cardiac glycoside, potently inhibits the Palytoxin (PTX)-induced K + release (IC50=0.42 μM) . Cymarin reveals an antitumor activity against breast cancer and pancreatic cancer . Cymarin exhibits antifeedant and growth inhibitory effects as crop protectant .
|
-
- HY-144683
-
-
- HY-14956
-
TG-873870
|
Antibiotic
Bacterial
|
Infection
Inflammation/Immunology
|
Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia .
|
-
- HY-148491
-
|
Others
|
Cancer
|
CSNK1-IN-2 is a CSNK1A1 inhibitor. CSNK1-IN-1 has inhibitory activity for CSNK1A1 kinase with IC50 values of 2.52 μM. CSNK1-IN-2 can be used for the research of proliferative disorders .
|
-
- HY-P4202
-
Suc-AEPF-pNA
|
Biochemical Assay Reagents
|
Others
|
Suc-Ala-Glu-Pro-Phe-pNA (Suc-AEPF-pNA) is a chromogenic substrate for the peptidylprolyl isomerase Pin1. Suc-Ala-Glu-Pro-Phe-pNA can be used to evaluate the inhibitory effect of the target compound on Pin1, and catalytic activity of Pin1, etc .
|
-
- HY-N11441
-
|
Phosphatase
|
Metabolic Disease
|
cis-Ferulic acid 4-O-β-D-glucopyranoside (compound 7) is a phenolic glycosid, which can be isolated from Nitraria sibirica.. cis-Ferulic acid 4-O-β-D-glucopyranoside exhibits antioxidant activity and potent inhibitory effect on Phosphatase PTP1B .
|
-
- HY-N4061
-
|
Interleukin Related
|
Inflammation/Immunology
|
Hedycoronen A has inhibitory activity on the IL-6, IL-12 p40, and TNF-α production in LPS-Stimulated BMDCs, with IC50s of 9.1 μM, 5.6 μM, and 46.0 μM. Hedycoronen A can be isolated from Hedychium coronarium .
|
-
- HY-P9921A
-
Ado-Trastuzumab emtansine (solution) ; PRO132365 (solution) ; T-DM 1 (solution)
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine). Trastuzumab emtansine can be used for the research of advanced breast cancer .
|
-
- HY-158570
-
|
Bacterial
|
Infection
|
(2E)-Eicosenoic acid is an inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase A (PtpA). (2E)-Eicosenoic acid exhibits strong inhibitory activity against PtpA with an IC50 value in the low micromolar range. (2E)-Eicosenoic acid can be used for research on Mycobacterium tuberculosis infection .
|
-
- HY-76648
-
|
HIV
|
Infection
|
NBD-556, a CD4 mimetic, is a potent HIV-1 entry inhibitor that blocks the gp120-CD4 interaction. NBD-556 shows potent cell fusion and virus-cell fusion inhibitory activity at low micromolar levels .
|
-
- HY-N0854
-
|
HBV
|
Infection
|
Alisol F is a triterpene isolated from Alisma orinentale, has immunosuppressive and anti-virus functions. Alisol F exhibits inhibitory activity in vitro on hepatitis B virus (HBV) surface antigen (HBsAg) secretion of the HepG2.2.15 cell line with an IC50 of 0.6 μM .
|
-
- HY-N1517
-
|
Aldose Reductase
|
Cancer
|
Ganoderic acid C2 is a bioactive triterpenoid in Ganoderma lucidum. Ganoderic acid C2 possesses the potential anti-tumor bioactivity, antihistamine, anti-aging and cytotoxic effects. Ganoderic acid C2 exhibits high inhibitory activity against the rat lens aldose reductase (RLAR) with an IC50 of 3.8 µM .
|
-
- HY-N0646
-
|
Phosphatase
Endogenous Metabolite
|
Cancer
|
Silydianin is an active constituent of Silybium marianum, with exhibit anti-collagenase, antitumor and anti-elastase activities. Silydianin is a natural protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 17.38 μM. Silydianin has inhibitory effect on the in vitro production and release of oxidative products .
|
-
- HY-103502
-
|
GABA Receptor
|
Neurological Disease
|
CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. CGP7930 enhances the inhibitory effect of l-baclofen on the oscillatory activity of cultured cortical neurons .
|
-
- HY-147940
-
|
Parasite
|
Infection
|
TbPTR1 inhibitor 1 (compound 5d) is a potent kinetoplastid pteridine reductase 1 (PTR1) inhibitor with an IC50<0.1 nM for TbPTR1. TbPTR1 inhibitor 1 has inhibitory activity against Trypanosoma brucei (EC50=0.66 μM) .
|
-
- HY-148200
-
|
ADC Cytotoxin
Telomerase
|
Cancer
|
L2H2-6OTD, containing one to four G-quadruplex binding loops, is a telomeric inhibitor analogue. l2H2-6OTD has telomerase inhibitory activity with an IC50 value of 15 nM .
|
-
- HY-162105
-
|
Cytochrome P450
|
Endocrinology
Cancer
|
Aromatase-IN-3 (compound 7d) is an aromatase inhibitor with an IC50 of 54 nM. Through suppressing the conversion of androstenedione to oestrogen caused by aromatase, Aromatase-IN-3 exerts an appreciable tumor growth inhibitory activities against breast cancer cell lines, suggesting its usage for ER+ cancer research .
|
-
- HY-157459
-
|
Fungal
|
Infection
|
SDH-IN-11 (compound A7) is a SDH inhibitor, and shows inhibitory effect on nematode feeding, reproductive ability, and egg hatching. SDH-IN-11 promotes the oxidative stress of nematodes and causes intestinal damage to nematodes. SDH-IN-11 inhibits the activity of succinate dehydrogenase (SDH) in nematodes .
|
-
- HY-126564
-
|
Lipase
MetAP
|
Others
Inflammation/Immunology
|
Ebelactone A is a mycolic acid β-lactone, which exhibits inhibitory activity for esterase, lipase, fMet aminopeptidase (fMet AP) and PNBase, with IC50s of 56, 3, 8 and 7.5 μM, respectively . Ebelactone A inhibits cutinase, exhibits plants protective potency against Erysiphe graminis .
|
-
- HY-160678
-
|
Bacterial
|
Infection
|
InhA-IN-7 (Compound 11) is a Triclocan (HY-B1119) derivative with inhibitory activity towards enoyl-acyl carrier protein reductase (InhA) with an IC50 of 96 nM. InhA-IN-7 inhibits proliferations of Mycobacterium tuberculosis wildtype and mutant strains with MICs ranging from 19 to 75 μM .
|
-
- HY-148200A
-
|
Telomerase
|
Cancer
|
L2H2-6OTD acetate contains one to four G-quadruplex binding loops and is a telomere inhibitor analog. L2H2-6OTD acetate has telomerase inhibitory activity with an IC50 value of 15 nM .
|
-
- HY-N12915
-
|
SHP2
Phosphatase
|
Metabolic Disease
Cancer
|
SHP2-IN-29 (Compound 3) is a potent SHP2 inhibitor with an IC50 value of 0.18 μM. SHP2-IN-29 also has inhibitory activity against PTP1B and TCPTP, with IC50 values of 4.27 and 4.74 μM, respectively.
|
-
- HY-118747
-
|
HIV
|
Infection
|
Scirpusin A is a naturally occurring compound extracted from the legume plant Caragana rosea Turcz, exhibiting anti-HIV activity. Scirpusin A demonstrates significant inhibitory effects against HIV-1 (EC50=7 μg/mL). Scirpusin A is utilized in research towards the development of anti-HIV therapeutics .
|
-
- HY-N0136S1
-
(±)-Dihydroquercetin-13C3
|
Autophagy
Tyrosinase
|
Inflammation/Immunology
|
(±)-Taxifolin-13C3 ((±)-Dihydroquercetin-13C3) is a derivative of (±)-Taxifolin, labeled with 13C3. (±)-Taxifolin is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
|
-
- HY-149896
-
|
Biochemical Assay Reagents
|
Cancer
|
Antitumor agent-107 (compound 5h) is an anticancer agent that shows excellent inhibitory activity against leukemia cell lines (GI50=0.32-1.34 μM). Antitumor agent-107 also shows antitumor activity against various other human cancer cell lines (GI50 range 0.35-9.43 μM) .
|
-
- HY-15392
-
|
ROCK
|
Cardiovascular Disease
|
Chroman 1 is a highly potent and selective ROCK inhibitor. Chroman 1 is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM). Chroman 1 also has inhibitory activity against MRCK, with an IC50 of 150 nM .
|
-
- HY-B0673
-
AMR69
|
TGF-beta/Smad
CCR
|
Inflammation/Immunology
Cancer
|
Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities .
|
-
- HY-16012
-
4SC-202
|
HDAC
Apoptosis
|
Cancer
|
Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
|
-
- HY-15392A
-
|
ROCK
|
Cardiovascular Disease
|
Chroman 1 dihydrochloride is a highly potent and selective ROCK inhibitor. Chroman 1 dihydrochloride is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM).
Chroman 1 dihydrochloride also has inhibitory activity against MRCK, with an IC50 of 150 nM .
|
-
- HY-144822
-
|
Bacterial
|
Infection
|
Anti-MRSA agent 2 (compound 14) has highly inhibitory activity against Methicillin-resistant Staphylococcus aureus (MRSA) with MIC of 0.098 μg/ml, and relatively low cytotoxicity in normal cells. Anti-MRSA agent 2 has strong ability to destroy bacterial membrane and bind to genomic DNA .
|
-
- HY-145655
-
|
CDK
|
Cancer
|
CDK7-IN-11 is an orally active CDK7 inhibitor. CDK7-IN-11 exhibits high CDK7 inhibitory activity with IC50 value of 4.2 nM. CDK7-IN-11 can be effectively used for the research of diseases associated with CDK7 .
|
-
- HY-152235
-
|
HDAC
|
Neurological Disease
Cancer
|
HDAC6-IN-15 is a selective histone deacetylase 6 (HDAC6) inhibitor. HDAC6-IN-15 has potent inhibitory activity for HDAC6 with IC50 value of 38.2 nM. HDAC6-IN-15 can be used for the research of cancer and neurodegenerative diseases .
|
-
- HY-P4202A
-
Suc-AEPF-pNA TFA
|
Biochemical Assay Reagents
|
Others
|
Suc-Ala-Glu-Pro-Phe-pNA (Suc-AEPF-pNA ) TFA is a chromogenic substrate for the peptidylprolyl isomerase Pin1. Suc-Ala-Glu-Pro-Phe-pNA TFA can be used to evaluate the inhibitory effect of the target compound on Pin1, and catalytic activity of Pin1, etc .
|
-
- HY-149813
-
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 14 (Compound 8a) is a high affinity P-gp inhibitor. P-gp inhibitor 14 reverses P-gp-mediated multidrug resistance (EC50=48.74 nM). P-gp inhibitor 14 has a weak inhibitory effect on CYP3A4 activity .
|
-
- HY-117002
-
|
Others
|
Cancer
|
SRI 37892 is a small molecule compound inhibitor of Frizzled protein 7 (Fzd7) with inhibitory activity against cancer cell proliferation (IC502μM). SRI 37892 significantly blocks Wnt/Fzd7 signaling. SRI 3789 can be used in the research of developing cancer therapeutic agents [1].
|
-
- HY-149610
-
|
Bacterial
|
Infection
|
Antibacterial agent 156 (Compound 57) is a selective and potent bactericidal against C. difficile and targets cell-wall synthesis. Antibacterial agent 156 exhibits bactericidal activity with the minimal inhibitory concentration of 0.5 μg/mL and 1 μg/mL against MIMIC50 (101 strains) and MIC90 (101 strains) .
|
-
- HY-N11999
-
|
Others
|
Others
|
5,4'-Dihydroxy-3,4,3'-trimethoxybibenzyl (compound 8) can be isolated from Dendrobium infundibulum (D. infundibulum). 5,4'-Dihydroxy-3,4,3'-trimethoxybibenzyl has no inhibitory activity against α-glucosidase and pancreatic lipase .
|
-
- HY-N0817
-
|
Apoptosis
Autophagy
Bacterial
|
Inflammation/Immunology
Cancer
|
Polyphyllin G is isolated from the rhizomes of Paris yunnanensis, with antimicrobial and anticancer activity. Polyphyllin G prevents the growth of both Gram-positive and Gram-negative bacteria with minimum inhibitory concentrations (MICs) .
Polyphyllin G induces apoptosis dependent on the activations of caspase-8, -3, and -9, induces autophagy .
|
-
- HY-157159
-
|
Btk
|
Cancer
|
BTK-IN-28 (compound PID-4) is a potent BTK inhibitor with anticancer activity. BTK-IN-28 has inhibitory effects on BTK and downstream signaling cascades and selectively inhibits Burkitt lymphoma RAMOS proliferation. BTK-IN-28 has no significant cytotoxicity towards non-tumor cells .
|
-
- HY-W017441
-
|
Others
|
Cancer
|
hUP1-IN-1 is a hUP1 inhibitor with Kii and Kis Urd of 375 and 635 nM. hUP1-IN-1 showes inhibitory activities over hUP1 catalyzed reaction with 70% at 1 μM. hUP1-IN-1 can be used for the research of cancer.
|
-
- HY-163429
-
|
TGF-β Receptor
p38 MAPK
|
Inflammation/Immunology
Cancer
|
J-1149 is a potent ALK5 inhibitor, with an IC50 value of 0.017 μM. J-1149 also shows weak p38α MAP kinase inhibitory activity, with an IC50 value of 0.435 μM. J-1149 can be used for liver fibrosis research .
|
-
- HY-B0319R
-
|
Fungal
Antibiotic
|
Infection
|
Tioconazole (Standard) is the analytical standard of Tioconazole. This product is intended for research and analytical applications. Tioconazole (UK-20349) is an antifungal imidazole derivative with broad spectrum activity. Tioconazole has inhibitory active aginst several dermatophytes and several yeasts with MIC50s <3.12 mg/L and <9 mg/L, respectively .
|
-
- HY-14356
-
-
- HY-157928
-
|
Keap1-Nrf2
|
Inflammation/Immunology
|
Keap1-Nrf2-IN-18 (Compound 22) is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor with good pharmacokinetics (PK) profiles and more potent in vivo activities in rats. Keap1-Nrf2-IN-18 has the strongest inhibitory activity in structure−activity relationship (SAR) study (KD = 0.0029 μM) .
|
-
- HY-13044
-
-
- HY-B0536
-
AM-1091; CI-960; PD 127391
|
Bacterial
Antibiotic
|
Infection
|
Clinafloxacin (AM 1091) is a potent and broad-spectrum fluoroquinolone antibiotic, has inhibitory activity against gram-positive, gram-negative bacterias, and anaerobic pathogens in vitro . Clinafloxacin is against DNA gyrase and topoisomerase IV of S. aureus with IC50 values of 0.92 µg/ml and 1.62 µg/ml, respectively .
|
-
- HY-16012A
-
4SC-202 free base
|
HDAC
Apoptosis
|
Cancer
|
Domatinostat (4SC-202 free base) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
|
-
- HY-B0778
-
|
Antibiotic
Parasite
|
Infection
|
Milbemycin oxime is an orally active macrolide with broad-spectrum antiparasitic activity. Milbemycin oxime is a mixture of oximes consisting of oxime derivatives corresponding to milbemycin A4 and A3. Milbemycin oxime binds to glutamate-gated chloride channels and has inhibitory potency against intestinal nematodes and lung/heart worms .
|
-
- HY-106888
-
|
Endogenous Metabolite
|
Neurological Disease
|
CS-722 Free base is a synthesized centrally acting muscle relaxant, and has a muscle relaxant activity and depressant effectson the spinal reflex . CS-722 Free base inhibits spontaneous inhibitory postsynaptic currents and excitatory postsynaptic currents in hippocampal cultures probably by an inhibition of both sodium and calcium currents .
|
-
- HY-B0536A
-
AM 1091 hydrochloride; CI 960 hydrochloride; PD127391 hydrochloride
|
Bacterial
Antibiotic
|
Infection
|
Clinafloxacin hydrochloride (AM 1091 hydrochloride) is a potent and broad-spectrum fluoroquinolone antibiotic, has inhibitory activity against gram-positive, gram-negative bacterias, and anaerobic pathogens in vitro . Clinafloxacin hydrochloride is against DNA gyrase and topoisomerase IV of S. aureus with IC50 values of 0.92 µg/ml and 1.62 µg/ml, respectively .
|
-
- HY-N3841
-
epsilon-Viniferin
|
Cytochrome P450
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
ε-Viniferin (epsilon-Viniferin), the dimer of Resveratrol and can be isolated from Vitis vinifera, displays a potent inhibitory for all the CYP activities, with Ki values from 0.5-20 μM. ε-Viniferin possesses potent antioxidant, anti-inflammatory, anti-diabetic, and anti-neurodegenerative capacity .
|
-
- HY-N0005S
-
-
- HY-103258
-
|
MAP3K
Apoptosis
|
Cancer
|
TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM) .
|
-
- HY-P0111
-
Z-WE(OMe)HD(OMe)-FMK
|
Caspase
Cathepsin
|
Cancer
|
Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis .
|
-
- HY-B0856
-
|
Fungal
Tyrosinase
Antibiotic
|
Infection
|
Validamycin A, a fungicidal, is an agricultural antibiotic. Validamycin A is originally isolated from Streptomyces hygroscopicus var. limoneus. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL . Validamycin A shows potent inhibitory activity against trehalase of Rhizoctonia solani, with an IC50 of 72 μM . Validamycin A is a reversible tyrosinase inhibitor, with a Ki of 5.893 mM .
|
-
- HY-109571
-
-
- HY-144065
-
|
Influenza Virus
|
Infection
|
Cap-dependent endonuclease-IN-19 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-19 is a spirocyclic pyridone derivative. Cap-dependent endonuclease-IN-19 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent CN111410661A, compound 1) .
|
-
- HY-N10335
-
|
FAK
|
Inflammation/Immunology
Cancer
|
Harringtonolide is a potent RACK1 inhibitor (IC50=39.66 μM in A375 cells). Harringtonolide inhibits the epithelial-mesenchymal transition (EMT) process and cell proliferation by affecting the interaction between FAK and RACK1. Harringtonolide has plant growth inhibitory, antiviral, anti-inflammatory, and antiproliferation activities .
|
-
- HY-146386
-
|
Sirtuin
|
Neurological Disease
Cancer
|
SIRT5 inhibitor 2 (compound 49) is a potent SIRT5 inhibitor with an IC50 value of 2.3 μM. SIRT5 inhibitor 2 has inhibitory activity against the SIRT5-dependent desuccinylation. SIRT5 inhibitor 2 can be used for researching cancer and neurodegenerative diseases .
|
-
- HY-147000
-
|
Bacterial
DNA/RNA Synthesis
|
Infection
|
DNA Gyrase-IN-1 (compound 42) is a potent and selective DNA gyrase inhibitor with an IC50 value of 2.6 µM. DNA Gyrase-IN-1 has high inhibitory activity against Mycobacterium tuberculosis (Mtb) with MIC of 0.49 µM. DNA Gyrase-IN-1 can be used for researching tuberculosis .
|
-
- HY-147746
-
|
MMP
|
Cancer
|
MMP2-IN-3 (compound 2) is a potent MMP-2 (matrix metalloproteinases) inhibitor, with an IC50 of 31 μM. MMP2-IN-3 also shows inhibitory activity against MMP-9 and MMP-8, with IC50 values of 26.6, and 32 μM, respectively .
|
-
- HY-151159
-
|
Dihydrofolate reductase (DHFR)
EGFR
|
Cancer
|
DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with an IC50 value of 123 nM. DHFR-IN-4 also has inhibitory activity against EGFR and HER2 with IC50s of 246 nM and 357 nM, respectively. DHFR-IN-4 has remarkable broad spectrum cytotoxic potency against cancer cells .
|
-
- HY-101679A
-
|
mAChR
|
Neurological Disease
|
YM-58790 free base is a potent antagonist of mAChR. YM-58790 free base binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 free base exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats .
|
-
- HY-126535
-
|
Glucosidase
|
Metabolic Disease
Cancer
|
Magnoloside B is an α-glucosidase inhibitor (IC50=0.69 mM), which can be obtained from Magnolia officinalis stem bark. Magnoloside B shows moderate inhibitory activity against MGC-803 and HepG2 cells. Magnoloside B has the potential to study cancer and diabetes .
|
-
- HY-19643
-
|
HCV Protease
|
Infection
|
JTK-109 is a potent inhibitor of hepatitis C virus NS5B RNA-dependent RNA polymerase. JTK-109 has NS5B inhibitory activity with IC50 value of 0.017μM. JTK-109 can be used for the research of hepatitis C virus (HCV) .
|
-
- HY-N12390
-
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
Alternaphenol B2 is a selective IDH1 inhibitor from the coral-derived fungus Parengyodontium album SCSIO SX7W11. Alternaphenol B2 shows inhibitory activity against isocitrate dehydrogenase mutant R132H (IDH1m), with IC50 values of 41.9 μM .
|
-
- HY-149676
-
|
Glucosidase
|
Metabolic Disease
|
α-Glucosidase-IN-42 (Compound 26) is a 9-O-berberrubine carboxylate derivative. α-Glucosidase-IN-42 has potent α-glucosidase inhibitory activities with an IC50 value in the range of 1.61 μM. α-Glucosidase-IN-42 can be used for the research of antidiabetic .
|
-
- HY-114846
-
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
Ro 22-9194 inhibits aggregation and thromboxane Az (TXA2) synthetase activity in rabbit and human platelets. Ro 22-9194 has a potent inhibitory action against various types of model arrhythmias. Ro 22-9194 has non-cholinergic cardiac depressant properties with its vasodilating action .
|
-
- HY-W017441A
-
|
Others
|
Cancer
|
hUP1-IN-1 potassium (compound 6a) is a hUP1 inhibitor with Kii and Kis Urd of 375 and 635 nM. hUP1-IN-1 potassium showes inhibitory activities over hUP1 catalyzed reaction with 70% at 1 μM. hUP1-IN-1 potassium can be used for the research of cancer .
|
-
- HY-161568
-
|
YAP
|
Cancer
|
TEAD-IN-10 (compound 15) has good selective activity and inhibitory effect on TEAD1 (IC50=14 nM), TEAD2 (IC50=179 nM) and TEAD3 (IC50=4 nnM) as a covalent inhibitor. TEAD-IN-10 can be used for cancer research .
|
-
- HY-114363A
-
|
c-Met/HGFR
|
Cancer
|
SRI 31215 (TFA) is a Matriptase/Hepsin/hepatocyte growth factor activator (HGFA) triplex inhibitor and mimics the activity of HAI-1/2 (endogenous inhibitors of HGF activation). SRI 31215 has potent inhibitory activity against matriptase, hepsin and HGFA with IC50 values of 0.69 μM, 0.65 μM and 0.30 μM, respectively. SRI 31215 can be used for the research of cancer .
|
-
- HY-155671
-
|
HDAC
|
Cancer
|
HDAC6-IN-18 (Compound 4) is a first irreversible HDAC6 isoform selective inhibitor with potent anti-multiple myeloma activity. HDAC6-IN-18 has HDAC6 inhibitory activity in RPMI8266, U266 and MM.1S cells with IC50 values of 0.17, 0.7 and 0.42 μM, respectively .
|
-
- HY-162242
-
|
Influenza Virus
|
Infection
|
Cap-dependent endonuclease-IN-27 (Compound 8) is an orally active potent cap-dependent endonuclease (CEN) inhibitor. Cap-dependent endonuclease-IN-27, an antiviral agent, shows activity against influenza B virus. Cap-dependent endonuclease-IN-27 has inhibitory activity against IFV A/WSN/33 (H1N1) polymerase (EC50 = 12.26 nM) .
|
-
- HY-161404
-
|
Bacterial
|
Infection
|
Antibacterial agent 202 (compound 45c) is a low cytotoxic bacterial inhibitor with good activity against Gram-negative bacteria, including Escherichia coli, Klebsiella pneumonia, especially Pseudomonas aeruginosa, (MIC (minimum inhibitory concentration)=7.8-31.25 μM). Antibacterial agent 202 can exert antibacterial activity by destroying the integrity of cell membranes and can be used in the research of bacterial infections .
|
-
- HY-125146
-
|
Others
|
Others
|
BMD4503-2 is a quinoxaline derivative with inhibitory activity against LRP5/6-sclerostin interactions. BMD4503-2 restores the activity of the Wnt/β-catenin signaling pathway by competitively binding to the LRP5/6-sclerostin complex. BMD4503-2 can be used in the study of Wnt signaling pathways in bone development, maintenance and osteoporosis .
|
-
- HY-13072
-
AS-703569; R-763
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
- HY-144659
-
|
Beta-lactamase
Apoptosis
Bacterial
|
Infection
|
Metallo-β-lactamase-IN-5 (compound 5c) is a potent metallo-β-lactamases (MBL) inhibitor. Metallo-β-lactamase-IN-5 shows inhibitory activity against MBLs NDM-1 and VIM-1. Metallo-β-lactamase-IN-5 inhibits HUVECs with an IC50 of 45 μg/mL. Metallo-β-lactamase-IN-5 plus Imipenem exhibits synergistic antimicrobial activity .
|
-
- HY-151422
-
|
Fungal
|
Infection
Cancer
|
Chitin synthase inhibitor 12 is a chitin synthase inhibitor. Chitin synthase inhibitor 12 shows excellent inhibitory activity with an IC50 value of 0.16 mM. Chitin synthase inhibitor 12 also is a broad-spectrum antifungal agent and has significantly antifungal activity against drug-resistant fungal variants, such as C. albicans and C. neoformans. Chitin synthase inhibitor 12 can be used for the research of invasive fungal infections (IFIs) .
|
-
- HY-151420
-
|
Fungal
|
Infection
Cancer
|
Chitin synthase inhibitor 10 is a chitin synthase inhibitor. Chitin synthase inhibitor 10 shows excellent chitin synthase inhibitory activity with an IC50 value of 0.11 mM. Chitin synthase inhibitor 10 also is an antifungal agent and has significantly antifungal activity against drug-resistant fungal variants, such as C. albicans and C. neoformans. Chitin synthase inhibitor 10 can be used for the research of invasive fungal infections (IFIs) .
|
-
- HY-151802
-
|
TrxR
|
Cancer
|
CPUL1 is a TrxR inhibitor, which shows proliferation-inhibitory and anti-metastatic activity against A549 cells. CPUL1 influences EMT (epithelial-mesenchymal transition) via inducing ROS-mediated ERK/JNK signaling by inhibiting TrxR1 enzyme activity. CPUL1 in combination with α-Lipoic Acid (HY-N0492) or Dithiodipropionic acid (HY-W014395) is more effective .
|
-
- HY-112661
-
Antibiotic PC-766B
|
Antibiotic
Bacterial
Fungal
|
Infection
Cancer
|
PC-766B is a macrolide antibiotic. PC-766B is active against Gram-positive bacteria, and some fungi and yeasts, but inactive against Gram-negative bacteria. PC-766B shows antitumor activity against murine tumor cells. PC-766B has weak inhibitory activity against Na +, K +-ATPase .
|
-
- HY-157389
-
|
Bcr-Abl
|
Cancer
|
AK-HW-90 (compound 2B) is a potent panBcr-Abl inhibitor with significant inhibitory activity against Imatinib (HY-15463)-resistant mutants. AK-HW-90 inhibits the resistance mutant Bcr-Abl T315I with an IC50 of 0.65 nM. AK-HW-90 has potential anticancer activity and can be used in the study of chronic myelogenous leukemia (CML) .
|
-
- HY-N0041
-
Gypenoside IV
|
NF-κB
COX
NO Synthase
|
Inflammation/Immunology
Cancer
|
Ginsenoside Rb3 is extracted from steamed Panax ginseng C. A. Meyer. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
|
-
- HY-18522
-
|
Phospholipase
|
Metabolic Disease
|
AA26-9 is a potent and broad spectrum serine hydrolase inhibitor. AA26-9 targets included serine peptidases, lipases, amidases, esterases, and thioesterases. AA26-9 shows inhibitory activity against approximately 1/3 of the 40+ serine hydrolases detected in immortalized T cell lines .
|
-
- HY-N0828
-
|
Autophagy
|
Inflammation/Immunology
Cancer
|
Pterostilbene is a stilbenoid isolated from blueberries and Pterocarpus marsupium . Shows anti-oxidant, anti-inflammatory, anti-carcinogenic, anti-diabetic and anti-obesity properties . Pterostilbene blocks ROS production , also exhibits inhibitory activity against various free radicals such as DPPH, ABTS, hydroxyl, superoxide and hydrogen peroxide .
|
-
- HY-103353
-
|
Cathepsin
Parasite
|
Infection
Cancer
|
SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G .
|
-
- HY-108351
-
|
Necroptosis
|
Cardiovascular Disease
|
IM-54 is a selective inhibitor of oxidative stress-induced necrosis. IM-54 shows potent inhibitory activity against H2O2-induced necrosis. IM-54 acts as a potential cardioprotective agent and biological tool for investigating the molecular mechanisms of cell death .
|
-
- HY-114672
-
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
MBCQ is a potent and selective cGMP-specific phosphodiesterase (PDE V; PDE5) inhibitor with an IC50 of 19 nM. MBCQ lacks inhibitory activity toward other PDE isozymes (all IC50s>100 μM). MBCQ dilates coronary arteries via specific inhibition of cGMP-PDE .
|
-
- HY-D0961
-
|
Wnt
|
Neurological Disease
|
Gallocyanine chloride, a synthetic blue dyestuff, blocks DKK1 inhibitory activity by disrupting DKK1/LRP6 interaction. Its association with LRP6 is weak (IC50 of about 3 μM in the inhibition of DKK1 binding). Gallocyanine dye acts as a potential agent for the research of Alzheimer's disease and related neurodegenerative tauopathies .
|
-
- HY-146299
-
|
Bacterial
|
Infection
|
Mt KARI-IN-2 (compound 5b) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 2.02 μM. Mt KARI-IN-2 has inhibitory activity against Mtb H37Rv (MIC = 0.78 μM) and low cytotoxicity (HEK IC50 > 86 μg/mL) .
|
-
- HY-146300
-
|
Bacterial
|
Infection
|
Mt KARI-IN-4 (compound 5c) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 5.48 μM. Mt KARI-IN-4 has inhibitory activity against Mtb H37Rv (MIC = 0.78 μM) and low cytotoxicity (HEK IC50 > 72 μg/mL) .
|
-
- HY-146301
-
|
Bacterial
|
Infection
|
Mt KARI-IN-5 (compound 6c) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 4.72 μM. Mt KARI-IN-5 has inhibitory activity against Mtb H37Rv (MIC = 1.56 μM) and low cytotoxicity (HEK IC50 > 64 μg/mL)
|
-
- HY-144335
-
|
DNA Alkylator/Crosslinker
|
Cancer
|
DNA crosslinker 2 (dihydrochloride) is a potent DNA minor groove binder with DNA binding affinity (ΔTm) of 1.2 °C. DNA crosslinker 2 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 2 (dihydrochloride) can be used for researching anticancer .
|
-
- HY-16566
-
Kanamycin A
|
Antibiotic
Bacterial
|
Infection
Inflammation/Immunology
|
Kanamycin (Kanamycin A) is an orally active antibacterial (gram-negative/positive bacteria) agent, inhibits translocation and causes misencoding by binding to the 70 S ribosomal subunit. Kanamycin shows good inhibitory activity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia .
|
-
- HY-151277
-
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
ALK5-IN-29 is an selective activin receptor-like kinase (ALK) inhibitor. ALK5-IN-29 can inhibit the activity of ALK5 with an IC50 value of ≤10 nM. ALK5-IN-29 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer .
|
-
- HY-152027
-
-
- HY-152028
-
|
HSP
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
HSP90-IN-19 is an effective heat shock protein 90 (Hsp90) inhibitor. HSP90-IN-19 has effective Hsp90 inhibitory activity with an IC50 value of 0.27 μM. HSP90-IN-19 can be used for the research of viral infection, neurodegenerative disease, and inflammation .
|
-
- HY-152032
-
|
Histone Demethylase
|
Cancer
|
LSD1-IN-23 is a competitive/non-competitive mixed inhibitor of lysine specific demethylase 1 (LSD1). LSD1-IN-23 has LSD1 inhibitory activity with an IC50 value of 0.58 μM. LSD1-IN-23 can be used for the research of neuroblastoma (NB) .
|
-
- HY-14585
-
Estrone 3-O-sulfamate
|
Steroid Sulfatase
|
Cancer
|
Estrone O-sulfamate (Estrone 3-O-sulfamate) is a potent steroid sulfatase (STS) inhibitor. Estrone O-sulfamate has inhibitory activity for STS in a placental microsomes (P.M.) preparation and in MCF-7 cells with IC50 values of 18 nM and 0.83 nM, respectively. Estrone O-sulfamate can be used for the research of cancer .
|
-
- HY-149817
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
AChE-IN-29, 3-OH pyrrolidine derivative, is an cholinesterase (ChE) inhibitor. AChE-IN-29 has cholinesterase inhibitory activity for hAChE, eeAChE and eqBChE with IC50 values of 0.25 μM, 0.23 μM and 0.72 μM, respectively. AChE-IN-29 can be used for the research of Alzheimer's disease .
|
-
- HY-N3348
-
|
Fungal
|
Infection
Inflammation/Immunology
|
Lyoniside is a lignan glycoside with antioxidant, allelopathic and antifungal activities, which can be isolated from the rhizomes and stems of bilberry (Vaccinium myrtillus L.). Lyoniside exhibits radical scavenging properties with an IC50 value of 23 μg/mL in DPPH assay. Lyoniside inhibits the mycelial growth of Fusarium oxysporum and Mucor hiemalis at 50 μg/mL with inhibitory rates of 78% and 80%, respectively .
|
-
- HY-155805
-
|
CDK
|
Cancer
|
CAF-382 (compound B1) is an analog of SNS-032 and a CDKL5 and pan-CDK inhibitor with a weak GSK3α/β affinity (>1.8 μM) and inhibitory activity. CAF-382 inhibits CDKL5 and blocks the phosphorylation of the CDKL5 E2 domain .
|
-
- HY-155668
-
|
HMG-CoA Reductase (HMGCR)
|
Metabolic Disease
|
HMG-CoA Reductase-IN-1 is a HMG-CoA reductase inhibitor. HMG-CoA Reductase-IN-1has high HMGR inhibitory activity and OATP1B1 affinity with pIC50 and pKm values of 8.54 and 1.98, respectively. HMG-CoA Reductase-IN-1 can be used for the research of hypercholesterolemia .
|
-
- HY-134008
-
|
Others
|
Cancer
|
Protoapigenone is an antineoplastic agent isolated from ferns. Protoapigenone has significant inhibitory activity against Hep G2, Hep 3B, MCF-7, A549 and MDAMB-231, with IC50s values of 1.60, 0.23, 0.78, 3.88 and 0.27 μg/mL respectively .
|
-
- HY-N12320
-
|
Antibiotic
|
Infection
|
Majoranaquinone exhibits a high antibacterial effect against 4 Staphylococcus, 1 Moraxella, and 1 Enterococcus strains. Majoranaquinone shows substantial efflux pump inhibitory activity in Escherichia coliATCC 25922 strain. Majoranaquinone is found to be an effective biofilm formation inhibitor on E.coli, ATCC 25922 and E. coli K-12 AG100 bacteria .
|
-
- HY-162237
-
|
RIP kinase
|
Inflammation/Immunology
|
RIPK1-IN-13 (compound 28) is a selective inhibitor for receptor-interacting serine/threonine-protein kinase 1 (RIPK1), the inhibitory activity is measured by ADP-Glo Kinase Assay with a pKi of 7.66. RIPK1-IN-13 inhibits human leukaemia cells U937 with a pIC50 of 7.2 .
|
-
- HY-163537
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
AChE/BuChE-IN-5 (compound 5a) is a dual target inhibitor. AChE/BuChE-IN-5 has excellent nanomolar inhibitory activity on acetylcholinesterase (AChE) (IC50=46.9 nM) and butyryl cholinesterase (BuChE) (IC50=3.5 nM). AChE/BuChE-IN-5 can be used for Alzheimer's Disease research .
|
-
- HY-W010995
-
|
Wnt
Survivin
β-catenin
|
Cancer
|
2,5-Dimethylcelecoxib is an analogue of celecoxib (HY-14398) with anticancer activity but without COX-2 inhibitory activity. 2,5-Dimethylcelecoxib exerts its anti-cancer cell proliferation effect by inhibiting the core mechanism of the Wnt/β-catenin signaling pathway. 2,5-Dimethylcelecoxib also inhibits T-cell factor-dependent transcriptional activity and inhibits expression of the Wnt/β-catenin target gene products cyclin D1 and survivin .
|
-
- HY-B1080R
-
|
HIF/HIF Prolyl-Hydroxylase
Influenza Virus
|
Infection
Neurological Disease
|
Tilorone (dihydrochloride) (Standard) is the analytical standard of Tilorone (dihydrochloride). This product is intended for research and analytical applications. Tilorone dihydrochloride is an orally active interferon (IFN) inducer with broad-spectrum antiviral activities. Tilorone dihydrochloride possesses robust anti-Severe fever with thrombocytopenia syndrome virus (SFTSV) activity in vitro and in vivo through stimulation of host innate immunity. Tilorone dihydrochloride can penetrate the blood-brain barrier to activate HIF in the CNS .Tilorone dihydrochloride exhibits an inhibitory activity with EC50 of 230 nM against Ebola virus (EBOV) .
|
-
- HY-11068
-
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
SB 239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC50 of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. SB 239063 has no effect on p38γ or p38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD .
|
-
- HY-12614
-
|
Glucokinase
|
Metabolic Disease
|
AMG-1694 is a potent glucokinase–glucokinase regulatory protein (GK-GKRP) disruptors and promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, indirectly increasing GK enzymatic activity. AMG-1694 potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation. AMG-1694 normalizes blood glucose levels in several rodent models of diabetes and lowes blood glucose restricted to diabetic and not normoglycaemic animals .
|
-
- HY-155131
-
|
Fungal
|
Infection
|
Y18501 is a oxysterol-binding protein (OSBPI) inhibitor with a similar structure to Oxathiapiprolin. Y18501 shows strong inhibitory activities against Phytophthora spp. and Pseudoperonospora cubensis, with EC50 ranging from 0.0005 to 0.0046 μg/mL. Y18501 shows excellent protective and curative activities against P. cubensis. Y18501 in combination with Chlorothalonil (HY-N6625) can significantly promote the inhibition of P. cubensis .
|
-
- HY-16566A
-
Kanamycin A sulfate
|
Bacterial
Antibiotic
|
Infection
|
Kanamycin (Kanamycin A) sulfate is an orally active antibacterial (gram-negative/positive bacteria) agent, inhibits translocation and causes misencoding by binding to the 70 S ribosomal subunit. Kanamycin sulfate shows good inhibitory activity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia .
|
-
- HY-100359
-
|
MMP
|
Inflammation/Immunology
Cancer
|
CL-82198 is a selective inhibitor of MMP-13. CL-82198 binds to the entire S1’ pocket of MMP-13, which is the basis for its selectivity towards MMP-13 and the lack of inhibitory activities against other MMPs . CL-82198 is a pharmacologic treatment for preventing osteoarthritis (OA) progression .
|
-
- HY-128338
-
|
CETP
|
Cardiovascular Disease
|
CETP-IN-3 (Compound 13) is an small molecule inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP. CETP-IN-3 for the CETP inhibitory activity in the scintillation proximity (SPA) and whole plasma assay (WPA) with IC50s of 0.002 μM and 0.06 μM, respectively .
|
-
- HY-N7110
-
|
Akt
ERK
JNK
|
Inflammation/Immunology
|
6-Hydroxyflavone is a naturally occurring flavone, with anti-inflammatory activity. 6-Hydroxyflavone exhibits inhibitory effect towards bovine hemoglobin (BHb) glycation. 6-Hydroxyflavone can activate AKT, ERK 1/2, and JNK signaling pathways to effectively promote osteoblastic differentiation. 6-Hydroxyflavone inhibits the LPS-induced NO production .
|
-
- HY-103353A
-
|
Cathepsin
Parasite
|
Infection
Cancer
|
SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 quarterhydrate shows no inhibitory activity against cathepsin G .
|
-
- HY-106961
-
ONO-AP 500-02
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
ONO 1301 (ONO-AP 500-02), a prostaglandin (PG) I2 mimetic, is an orally active, long-acting prostacyclin agonist with thromboxane-synthase inhibitory activity. ONO 1301 promotes production of hepatocyte growth factor (HGF) from various cell types and ameliorates ischemia-induced left ventricle dysfunction in the mouse, rat and pig .
|
-
- HY-145426
-
|
HDAC
|
Cancer
|
MPT0B390 is an arylsulfonamide-based derivative with potent HDAC inhibitory ability. MPT0B390, TIMP3 inducer, inhibits tumor growth, metastasis and angiogenesis. MPT0B390 shows antiproliferative activity against human colon cancer cell line HCT116 with the GI50 of 0.03 μM .
|
-
- HY-144284
-
|
Bacterial
|
Infection
|
MsbA-IN-5 (compound 40) is a potent and highly selective MsbA inhibitor with an IC50 value of 2 nM. MsbA-IN-5 has inhibitory activity against Escherichia coli, Klebsiella pneumoniae, and Enterobacter cloacae with MICs of 12 μM, 12 μM and 25 μM, respectively. MsbA-IN-5 can be used for researching anti-Gram-negative bacteria .
|
-
- HY-143456
-
|
Others
|
Inflammation/Immunology
|
Anti-inflammatory agent 18 (compound 3b) shows NO inhibitory activity, with an IC50 of 15.94 μM. Anti-inflammatory agent 18 inhibits HMGB1-induced later inflammation. Anti-inflammatory agent 18 can be used for the research of later inflammation diseases such as coronavirus diseases (COVID-19) and sepsis, etc .
|
-
- HY-143457
-
|
Others
|
Inflammation/Immunology
|
Anti-inflammatory agent 19 (compound 2b) shows NO inhibitory activity, with an IC50 of 36.00 μM. Anti-inflammatory agent 19 inhibits HMGB1-induced later inflammation. Anti-inflammatory agent 19 can be used for the research of later inflammation diseases such as coronavirus diseases (COVID-19) and sepsis, etc .
|
-
- HY-144823
-
|
Bacterial
|
Infection
|
Anti-MRSA agent 3 (compound 18) has highly inhibitory activity against Methicillin-resistant Staphylococcus aureus (MRSA) with MIC of 0.098 μg/ml, and low cytotoxicity in normal cells. Anti-MRSA agent 3 has relatively strong ability to destroy bacterial cell wall and membrane, high binding affinity to bacterial genomic DNA .
|
-
- HY-151376
-
|
Proteasome
|
Infection
|
SAP2-IN-1 is a secreted aspartic protease 2 (SAP2) inhibitor and has potent SAP2 inhibitory activity with an IC50 value of 0.92 μM. SAP2-IN-1 also is a virulence factor inhibitor and is inactive in vitro. SAP2-IN-1 can be used for the research of infection .
|
-
- HY-14956S
-
TG-873870-d3
|
Bacterial
|
Inflammation/Immunology
|
Nemonoxacin-d3 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia[1][2][3].
|
-
- HY-14956S2
-
TG-873870-d4
|
Bacterial
|
Inflammation/Immunology
|
Nemonoxacin-d4 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia[1][2][3].
|
-
- HY-153989
-
|
Ras
Cytochrome P450
|
Cancer
|
SOS1-IN-16 (Comp 54) is a selective inhibitor of SOS1 with an IC50 of 7.2 nM. SOS1-IN-16 has inhibitory activity of CYP3A4 when using testosterone as a substrate, with an IC50 of 8.9μM. SOS1-IN-16 can be used for cancer research .
|
-
- HY-149634
-
|
PI3K
|
Cancer
|
PI3Kδ-IN-17 (Compound S5) is a potent inhibitor of PI3Kδ, with IC50 of 2.82?nM. PI3Kδ-IN-17 shows strong inhibitory activity of proliferation in SU-DHL-6 cells (IC50 = 0.035 μM) .
|
-
- HY-160111
-
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
PDM-042 is a potent, selective, and orally active phosphodiesterase 10A (PDE10A) inhibitor. PDM-042 shows potent inhibitory activities for human and rat PDE10A with IC50 values of less than 1 nM and more than 1000-fold selectivity against other phosphodiesterases. PDM-042 can be used for the research of schizophrenia .
|
-
- HY-158338
-
|
MAGL
|
Others
Neurological Disease
Inflammation/Immunology
Cancer
|
ABHD antagonist 1 possesses ABHD6 (α/β-Hydrolase domain containing 6) inhibitory activity, involving the regulation of biochemical pathways involved in ABHD6, thereby affecting cell function and inflammatory response. ABHD antagonist 1 can be used in pain, neuropathic diseases, inflammatory diseases. Autoimmune diseases, metabolic diseases, and cancer research .
|
-
- HY-B0648
-
17α-Hydroxy-6α-methylprogesterone; U8840
|
Progesterone Receptor
|
Endocrinology
Cancer
|
Medroxyprogesterone (17α-Hydroxy-6α-methylprogesterone) is a synthetic human variant of progesterone that is a progesterone receptor agonist with oral activity. Medroxyprogesterone can induce cell proliferation through the PI3K/Akt signaling pathway. Medroxyprogesterone has an inhibitory effect on atherosclerosis in mice. The progesterone agonist activity of Medroxyprogesterone is less effective than Medroxyprogesterone acetate (HY-B0469) .
|
-
- HY-10235S
-
VX-950-d4
|
Isotope-Labeled Compounds
HCV Protease
HCV
SARS-CoV
|
Infection
|
Telaprevir-d4 is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide[1][2][3]. Telaprevir inhibits SARS-CoV-2 3CLpro activity[4].
|
-
- HY-143236
-
|
Bacterial
Fungal
|
Infection
|
DHFR-IN-1 (compound 12) is a potent and selective DHFR (dihydrofolate reductase)inhibitor, with an IC50 of 40.71 nM. DHFR-IN-1 exhibits promising antibacterial activity against gram-positive and gram-negative bacteria. DHFR-IN-1 exhibits moderate antifungal activities. DHFR-IN-1 exhibits a high synergistic effect with Levofloxacin (HY-B0330), where the FIC (fractional inhibitory concentration index) value is 0.249 .
|
-
- HY-152037
-
|
Cholinesterase (ChE)
Keap1-Nrf2
|
Neurological Disease
|
AChE/Nrf2 modulator 1 is an orally active acetylcholinesterase (AChE)/nuclear factor erythroid 2-related factor 2 (Nrf2) modulator. AChE/Nrf2 modulator 1 has Nrf2 inductive activity and AChE inhibitory activity for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively. AChE/Nrf2 modulator 1 can be used for the research of Alzheimer's disease .
|
-
- HY-156965
-
|
Others
|
Metabolic Disease
Cancer
|
BAY-771, a structurally close pyrimidinedione, is a chemical probe with good lead-like properties and high permeability in Caco-2 cells (no hint of efflux). BAY-771 shows very weak inhibitory activity in the BCAT1 biochemical assay and no activity in BCAT2. BAY-771 can be used as a negative control of HY-148242 BAY-069. BAY-771 can be used for the research of tumor metabolism .
|
-
- HY-N6257
-
|
ERK
PGE synthase
COX
NF-κB
|
Inflammation/Immunology
Cancer
|
Cafestol, one of the major components of coffee, is a coffee-specific diterpene from. Cafestol is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activation pathway. Cafestol contributes to its beneficial effects through various biological activities such as chemopreventive, antitumorigenic, hepatoprotective, antioxidative and antiinflammatory effects .
|
-
- HY-32219
-
|
Acyltransferase
|
Metabolic Disease
|
T863 is an orally active, selective and potent DGAT1 (acyl-CoA:diacylglycerol acyltransferase 1) inhibitor with an IC50 of 15 nM. T863 has no inhibitory activity against human MGAT3, human DGAT2, or human MGAT2. T863 interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells .
|
-
- HY-13402
-
LY315920
|
Phospholipase
|
Inflammation/Immunology
|
Varespladib (LY315920) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively .
|
-
- HY-13402A
-
LY315920 sodium
|
Phospholipase
|
Inflammation/Immunology
|
Varespladib sodium (LY315920 sodium) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib sodium exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively .
|
-
- HY-18307
-
|
c-Met/HGFR
|
Cancer
|
SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC50s of 4 and 9 nM, respectively. SYN1143 has weak inhibitory activity on Lck, Tie2, Src, and BTK with IC50s ranging from 160 to 710 nM. SYN1143 can be used for the research of cancers that RON and c-Met are activated .
|
-
- HY-N3243
-
-
- HY-N3244
-
-
- HY-110167
-
|
PGE synthase
Ligands for Target Protein for PROTAC
|
Cancer
|
TFC-007, a selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, show high inhibitory activity against H-PGDS enzyme (IC50 value of 83 nM). TFC-007 can be used for composing H-PGDS degradation inducer PROTAC(H-PGDS)-1 (TFC-007 binds to H-PGDS, and Pomalidomide binds to cereblon) .
|
-
- HY-105793
-
|
mAChR
|
Neurological Disease
|
Mazaticol is an anticholinergic agent. Mazaticol blocks the muscarinic acetylcholine receptors and cholinergic nerve activity. Mazaticol is a potent 3H-QNB and 3H-PZ binding inhibitor, can bind to the M2 receptors with high affinity. Mazaticol exhibits inhibitory effects on dopamine uptake in the striatal nerve terminal. Mazaticol can be used for parkinsonian syndrome research .
|
-
- HY-147794
-
|
COX
|
Cancer
|
COX-2-IN-18 (Compound 3) is a potent inhibitor of COX-2. COX-2-IN-18 possesses good COX-2 inhibitory activity (IC50 = 0.775 μM) compared to the reference agent, Celecoxib (IC50 = 0.153 μM). COX-2-IN-18 has the potential for the research of cancer diseases .
|
-
- HY-147745
-
|
MMP
|
Cancer
|
MMP2-IN-2 (compound 42) is a potent and selective MMP-2 (matrix metalloproteinases) inhibitor, with an IC50 of 4.2 μM. MMP2-IN-2 also shows inhibitory activity against MMP-13, MMP-9 and MMP-8, with IC50 values of 12, 23.3, and 25 μM, respectively .
|
-
- HY-N1636
-
|
Monoamine Oxidase
|
Neurological Disease
|
1-Methyl-2-nonyl-4(1H)-quinolone, a quinolone alkaloid, is a potent and selective MAO-B (monoamine oxidase) inhibitor. 1-Methyl-2-nonyl-4(1H)-quinolone exhibites inhibitory activity on leukotriene biosynthesis, with an IC50 of 12.1 μM .
|
-
- HY-N7844
-
Benzyladenosine
|
Apoptosis
Adenosine Receptor
|
Inflammation/Immunology
Cancer
|
N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma - .
|
-
- HY-150577
-
|
HDAC
|
Cancer
|
HDAC-IN-45 (Compound 14) is a small molecule HDAC inhibitor and has anticancer activity, also can forms a hydrogen
bond with residue Y303. HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms with IC50 values of 0.108, 0.585 and 0.563 μM respectively .
|
-
- HY-146213
-
|
CDK
|
Cancer
|
CDK4/6-IN-12 is a potent cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. CDK4/6-IN-12 has enzymatic inhibitory activity for CDK4 and CDK6 with IC50 of 592.3 nM and 3090 nM, respectively. CDK4/6-IN-12 can be used for the research of cancer .
|
-
- HY-151289
-
|
TGF-β Receptor
TGF-beta/Smad
|
Cancer
|
ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC50 value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer .
|
-
- HY-151358
-
|
Others
|
Cancer
|
SENP2-IN-1 (compound 77) is a selective SENP2 inhibitor. SENP2-IN-1 shows inhibitory activities with IC50s of 1.3, 0.69 and 22.7 μM for SENP1, SENP2 and SENP5, respectively. SENP2-IN-1 can be used for the research of cancer .
|
-
- HY-14956S1
-
TG-873870-d3-1
|
Bacterial
|
Inflammation/Immunology
|
Nemonoxacin-d3-1 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia[1][2][3].
|
-
- HY-149273
-
|
Cholinesterase (ChE)
Amyloid-β
Tau Protein
|
Neurological Disease
|
hBChE-IN-1 (compound 4), a quinolizidinyl derivative, is a potent hBChE inhibitor (IC50=7 nM) and highly selective over hAChE. hBChE-IN-1 shows inhibitory activity against tau and Aβ40 protein aggregation, with IC50 values of 20 and 4.3 μM, respectively. hBChE-IN-1 can be used for Alzheimer's disease research .
|
-
- HY-103295
-
|
Bradykinin Receptor
|
Metabolic Disease
Inflammation/Immunology
|
Lys-[Des-Arg9]Bradykinin, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin has low inhibitory activity on B2 receptors .
|
-
- HY-N7160
-
|
Src
Apoptosis
|
Cancer
|
2-Hydroxy-3-methylanthraquinone (compound 1) is a natural compound isolated from a water extract of Hedyotis diffusa WILLD. 2-Hydroxy-3-methylanthraquinone shows inhibitory activity against protein tyrosine kinases v-src and pp60src, and induces growth arrest and apoptosis in the HepG2 cancer cells .
|
-
- HY-N3841A
-
|
Cytochrome P450
|
Metabolic Disease
|
δ-Viniferin is a resveratrol dehydrodimer, an isomer of ε-Viniferin (HY-N3841) . ε-Viniferin (epsilon-Viniferin), the dimer of Resveratrol, displays a potent inhibitory for all the CYP activities, with Ki values from 0.5-20 μM. ε-Viniferin possesses potent antioxidant, anti-inflammatory, anti-diabetic, and anti-neurodegenerative capacity.
|
-
- HY-N7150
-
5,7-Dihydroxy-3',4',5'-trimethoxyflavone
|
Xanthine Oxidase
|
Metabolic Disease
|
Tricetin 3',4',5'-trimethyl ether (5,7-Dihydroxy-3',4',5'-trimethoxyflavone) is a flavone glucoside, that can be isolated the flowers of Chrysanthemum sinensea. Tricetin 3',4',5'-trimethyl ether displays xanthine oxidase competitive-type inhibitory activity, with an IC50 of 0.51 μM and a Ki of 0.37 μM .
|
-
- HY-N12726
-
|
p38 MAPK
MMP
|
Infection
Inflammation/Immunology
Cancer
|
Halociline, a derivative of alkaloids, that can be isolated from the marine fungus Penicillium griseofulvum.
Halociline targets MAPK1, MMP-9, and PIK3CA in gastric cancer cells, potentially mediated by diverse pathways including cancer, lipid metabolism, atherosclerosis, and EGFR tyrosine kinase inhibitor resistance. Halociline possesses antimicrobial, antioxidant and biofilm inhibitory activities .
|
-
- HY-158166
-
|
DNA-PK
|
Inflammation/Immunology
Cancer
|
DNA-PK-IN-13 (Compound SK10) is a DNA-PK inhibitor that exhibits potent inhibitory activity (IC50= 0.11 nM). DNA-PK-IN-13 regulates tumor cell proliferation by decreasing the expression level of γH2A.X and enhancing the sensitivity of tumor cells to chemotherapeutic agents. DNA-PK-IN-13 is suitable for oncology studies .
|
-
- HY-P6177
-
|
Dipeptidyl Peptidase
|
Inflammation/Immunology
|
SGP8 (IAVPGEVA) is an octopeptide derived from the hydrolysis of soybean 11S globulin. SGP8 (IAVPGEVA) has the role of regulating lipid metabolism, inflammation and fibrosis. SGP8 (IAVPGEVA) exhibits inhibitory activity against DPP4 and inhibits the JNK-c-Jun signaling pathway. SGP8 (IAVPGEVA) has the ability to inhibit the non-alcoholic steatohepatitis (NASH) .
|
-
- HY-14956R
-
|
Antibiotic
Bacterial
|
Infection
Inflammation/Immunology
|
Nemonoxacin (Standard) is the analytical standard of Nemonoxacin. This product is intended for research and analytical applications. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia .
|
-
- HY-161611
-
|
Others
|
Others
|
Plant 14-3-3-IN-1 (Compound 2) is an inhibitor for 14-3-3 proteins in Arabidopsis thaliana, with an IC50 of 1.21 μM. Plant 14-3-3-IN-1 exhibits different inhibitory activities against different 14-3-3 isomers. Plant 14-3-3-IN-1 promotes the closure of stomata on leaves .
|
-
- HY-163659
-
|
Influenza Virus
|
Infection
|
Anti-Influenza agent 6 (compound 19b) shows inhibitory activity against A/WSN/33/H1N1 (EC50 = 0.015 μM) and influenza B virus Yamagata/16/88 (EC50 = 0.073 μM) and Victotis/2/87 (EC50 = 0.067 μM) .
|
-
- HY-13269
-
|
HIV
HIV Integrase
|
Infection
Inflammation/Immunology
|
BMS-707035 is a potent orally active HIV-1 integrase strand transfer inhibitor (INSTI). BMS-707035 has enzyme inhibitory with an IC50 value of 3 nM. BMS-707035 also has weak CYP inhibiton and antiviral activity. BMS-707035 can be used for the research of human immunodeficiency virus-1 (HIV-1) .
|
-
- HY-13334
-
NVP-BGT226 maleate
|
PI3K
mTOR
Autophagy
Apoptosis
|
Cancer
|
BGT226 (NVP-BGT226 maleate) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ) /mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells .
|
-
- HY-18010
-
|
Btk
BCRP
|
Inflammation/Immunology
|
PCI 29732 is a potent, orally active, reversible BTK inhibitor with Ki app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 .
|
-
- HY-N2284
-
|
Cholinesterase (ChE)
Beta-secretase
Phosphodiesterase (PDE)
|
Cancer
|
Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC50 of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 µM, 0.17 µM, 17.89 µg/mL, 10.98 µM, 8.37 µM and 8.21 µM, respectively.
|
-
- HY-101664
-
IY-81149
|
Proton Pump
TOPK
|
Inflammation/Immunology
Cancer
|
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-122198
-
|
Others
|
Cancer
|
ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation .
|
-
- HY-103295A
-
|
Bradykinin Receptor
|
Metabolic Disease
Inflammation/Immunology
|
Lys-[Des-Arg9]Bradykinin TFA, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin TFA has low inhibitory activity on B2 receptors .
|
-
- HY-13334A
-
NVP-BGT226
|
PI3K
mTOR
Autophagy
|
Cancer
|
BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ)/mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells .
|
-
- HY-138565
-
|
YAP
|
Cancer
|
K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma .
|
-
- HY-150639
-
|
Raf
|
Cancer
|
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma .
|
-
- HY-N1735
-
|
Others
|
Inflammation/Immunology
|
2′-Hydroxygenistein is a natural product that can be isolated from Crotalaria pallida and C. assamica. 2′-Hydroxygenistein shows anti-inflammatory activity. 2′-Hydroxygenistein shows significant concentration-dependent inhibitory effects on the release of β-glucuronidase and lysozyme from rat neutrophils, with IC50 values of 5.9 ± 1.4 and 9.7 ± 3.5 μM, respectively .
|
-
- HY-155032
-
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity,and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015),inhibits tumor progress in nude mice KBV xenograft tumors model .
|
-
- HY-156759
-
|
METTL3
|
Cancer
|
METTL3-IN-5 (Compound 13) is a METTL3 inhibitor. METTL3-IN-5 inhibits MOLM-13 growth with an IC50 less than 2 μM. METTL3-IN-5 has weak hERG inhibitory activity (IC50 >30 μM). METTL3-IN-5 can be used for AML research .
|
-
- HY-157298
-
|
Apoptosis
|
Cancer
|
anti-TNBC agent-4 (compound 7) exhibits highly inhibitory activity against different TNBC cells with IC50s from 0.37 μM to 1.52 μM. anti-TNBC agent-4 inhibits IKKβ mediated phosphorylation of IκB and p65. anti-TNBC agent-4 induces TNBC cells apoptosis .
|
-
- HY-160597
-
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
Exatecan-amide-bicyclo[1.1.1]pentan-1-ol (Compound 79) is an exatecan (HY-13631) derivative that can be used as a payload in drug conjugates. Exatecan-amide-bicyclo[1.1.1]pentan-1-ol has significant inhibitory activity against a variety of tumor cell lines .
|
-
- HY-B0673R
-
|
TGF-beta/Smad
CCR
|
Inflammation/Immunology
Cancer
|
Pirfenidone (Standard) is the analytical standard of Pirfenidone. This product is intended for research and analytical applications. Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities .
|
-
- HY-N0632
-
|
COX
NF-κB
|
Inflammation/Immunology
|
Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta .
Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models , has selective inhibitory activity towards cyclooxygenase-2 (COX-2) .
Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways .
|
-
- HY-N6924
-
|
HIV
|
Infection
Metabolic Disease
|
Zingibroside R1 is dammaranae-type triterpenoid saponin, isolated from rhizomes, taproots, and lateral roots of Panax japonicas C. A. Meyer, shows excellent anti-tumor effects as well as anti-angiogenic activity .
Zingibroside R1 possesses some anti-HIV-1 activity.
Zingibroside R1 has inhibitory effects on the 2-deoxy-D-glucose (2-DG) uptake by EAT cells (IC50=91.3 μM) .
|
-
- HY-125798
-
Neu5Ac2en; DANA
|
Influenza Virus
|
Infection
|
N-acetyl-2,3-dehydro-2-Deoxyneuraminic Acid (Neu5Ac2en) is a potent neuraminidase (sialidase) inhibitor. N-acetyl-2,3-dehydro-2-Deoxyneuraminic Acid shows inhibitory activities against human neuraminidase enzymes with IC50s of 143, 43, 61, and 74 μM for NEU1, NEU2, NEU3, and NEU4, respectively. Anti-influenza virus activity .
|
-
- HY-146208
-
|
Epigenetic Reader Domain
|
Cancer
|
BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer .
|
-
- HY-163065
-
|
Opioid Receptor
Sigma Receptor
|
Neurological Disease
|
σ1 Receptor/μ Opioid receptor modulator 2 (compound 4x) is a dual μOR agonist/σ1R antagonist, and displays picomolar μOR agonism activity (EC50: 0.6 ± 0.2 nM) and good σ1R inhibitory activity (Ki: 363.7 ± 5.6 nM). σ1 Receptor/μ Opioid receptor modulator 2 exhibits robust analgesic effects in various pain models .
|
-
- HY-161366
-
|
PI3K
|
Cancer
|
OMS14 is exhibits inhibitory activity for phosphoinositide 3-kinase γ (PI3Kγ) and PIK3CD/PIK3R1, which inhibits 19% PI3Kγ and 65% PIK3CD/PIK3R1 activity at 100 μM. OMS14 exhibits anticancer efficacy in various cancer cells .
|
-
- HY-10235
-
VX-950
|
HCV Protease
HCV
SARS-CoV
|
Infection
|
Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide . Telaprevir inhibits SARS-CoV-2 3CL pro activity .
|
-
- HY-15147
-
|
β-catenin
PARP
|
Cancer
|
XAV-939 is a Tankyrase inhibitor. XAV-939 has inhibitory activity for TNKS1 and TNKS2 with IC50 values of 5 nM and 2 nM, respectively. XAV-939 also is an enhancer of osteoblastic differentiation of hMSCs. XAV-939 can be used for the research of conditions associated with activated Wnt signaling, such as cancer, fibrotic diseases and conditions associated with low bone formation .
|
-
- HY-124618
-
|
Flavivirus
Dengue virus
HCV
HIV
|
Infection
|
FGI-106 is a potent and broad-spectrum inhibitor with inhibitory activity against multiple viruses. FGI-106 is active against Ebola, Rift Valley and Dengue Fever viruses with EC50s of 100 nM, 800 nM and 400-900 nM, respectively. FGI-106 also inhibits non-hemorrhagic fever viruses HCV and HIV-1 with EC50s of 200 nM and 150 nM, respectively .
|
-
- HY-143325
-
|
HDAC
Adenosine Receptor
|
Cancer
|
A2AAR/HDAC-IN-2 is a potent A2AAR/HDAC dual inhibitor, with good binding affinity for A2AAR (Ki=10.3 nM) and good inhibitory activity against HDAC1 (IC50=18.5 nM). A2AAR/HDAC-IN-2 can be used in study of antitumor .
|
-
- HY-151933
-
|
HIV
Reverse Transcriptase
|
Infection
|
HIV-1 inhibitor-49 is an orally active HIV-1 inhibitor, is a HEPT analog. HIV-1 inhibitor-49 possesses great pharmacokinetics profiles and potent non-nucleoside reverse transcriptase inhibitory activity (IC50=30 nM). HIV-1 inhibitor-49 exerts potential safety without acute toxicity in mouse model .
|
-
- HY-155114
-
|
HIV
|
Infection
|
HIV-1 inhibitor-59 (Compound I-5b) is a HIV-1 inhibitor, with EC50s of 5.62-171 nM against the wild-type (WT) and mutant HIV-1 strains. HIV-1 inhibitor-59 has moderate RT enzyme inhibitory activity (IC50: 0.094-12.0 μM) .
|
-
- HY-48517
-
|
Others
|
Cancer
|
L2H2-6OTD intermediate-1 is an intermediate for the synthesis of L2H2-6OTD (HY-148200) and can be used for ADC preparation. L2H2-6OTD, a telomestatin analog with telomerase inhibitory activity (IC50: 15 nM) [1] .
|
-
- HY-163094
-
|
EGFR
|
Cancer
|
EGFR-IN-95 (compound 5j) is an 2,4-diaminonicotinamide derivative. EGFR-IN-95 has potent inhibitory activity against EGFR del19/T790M/C797S and L858R/T790M/C797S .
|
-
- HY-48626
-
|
Others
|
Others
|
L2H2-6OTD intermediate-3 is an intermediate for the synthesis of L2H2-6OTD (HY-148200) and can be used for ADC preparation. L2H2-6OTD, a telomestatin analog with telomerase inhibitory activity (IC50: 15 nM) .
|
-
- HY-B0536R
-
|
Bacterial
Antibiotic
|
Infection
|
Clinafloxacin (Standard) is the analytical standard of Clinafloxacin. This product is intended for research and analytical applications. Clinafloxacin (AM 1091) is a potent and broad-spectrum fluoroquinolone antibiotic, has inhibitory activity against gram-positive, gram-negative bacterias, and anaerobic pathogens in vitro . Clinafloxacin is against DNA gyrase and topoisomerase IV of S. aureus with IC50 values of 0.92 µg/ml and 1.62 µg/ml, respectively .
|
-
- HY-13766A
-
VX-853-2
|
Others
|
Others
|
Timcodar mesylate (VX-853-2) and its analog VX-710 are mammalian multidrug-resistant bacterial efflux pump inhibitors that directly inhibit ethidium bromide efflux in Staphylococcus aureus. Timcodar mesylate has the potential to enhance antibiotic activity by inhibiting bacterial efflux pumps, effectively reducing the minimum inhibitory concentration of some antibiotics against Gram-positive pathogens such as Staphylococcus aureus, Enterococcus and Streptococcus pneumoniae .
|
-
- HY-158409
-
|
Molecular Glues
Ras
|
Cancer
|
Pan-rasin-2 (compound 6A) is a molecular glues that targets RAS. Pan-rasin-2 has significant inhibitory activity on cell proliferation of RAS mutant cell lines. Pan-rasin-2 can form ternary complexes with cyclophilin A (CYPA) and RAS (ON) proteins and the formation of ternary complexes can block the binding of RAF downstream of RAS, which has anti-tumor effects .
|
-
- HY-B1138
-
CL-82204
|
COX
Caspase
|
Inflammation/Immunology
|
Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor .
|
-
- HY-146461
-
|
Apoptosis
Caspase
ROS Kinase
|
Cancer
|
Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model .
|
-
- HY-150026
-
|
VEGFR
PDGFR
FGFR
c-Kit
Akt
Src
Apoptosis
|
Cancer
|
Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity .
|
-
- HY-119213
-
|
Influenza Virus
|
Infection
|
BMY-27709 is an influenza virus growth inhibitor with an IC50 value of 3-8 μM against A/WSN/33 virus growth, and also exhibits inhibitory activity against some subtypes of influenza viruses. BMY-27709 acts early in the course of H1 and H2 virus infections, and exhibits antiviral activity through inhibition of hemagglutinin proteins. However, BMY-27709 has no effect on H3 subtype viruses and influenza B/Lee/40 viruses .
|
-
- HY-137355
-
15(S)-15-Methyl PGD2
|
Prostaglandin Receptor
|
Metabolic Disease
|
15(S)-15-methyl Prostaglandin D2 (15(S)-15-methyl PGD2) is a metabolically stable synthetic analog of PGD2. In contrast to PGD2, 15(S)-15-methyl PGD2 induces vasoconstriction and increases systemic blood pressure with much reduced inhibitory activity on ADP-induced platelet aggregation. It also exhibits strong antifertility activity in hamsters (200-fold more potent than PGD2).
|
-
- HY-15160
-
TAK-960
2 Publications Verification
|
Polo-like Kinase (PLK)
|
Cancer
|
TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-19340
-
TMS
5 Publications Verification
(E)-2,3',4,5'-tetramethoxystilbene
|
Cytochrome P450
|
Cancer
|
TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive CYP1B1 inhibitor with an IC50 of 6 nM and a Ki value of 3 nM. TMS shows a lesser extent inhibitory effect on CYP1A1 (IC50=300 nM) and CYP1A2 (IC50=3.1 μM). TMS is a methylated derivative of resveratrol and has anti-cancer activity .
|
-
- HY-15160B
-
|
Polo-like Kinase (PLK)
|
Cancer
|
TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-N4215
-
|
Others
|
Inflammation/Immunology
|
11(α)-Methoxysaikosaponin F is a triterpenoid saponin isolated from Bupleurum marginatum Wall.ex DC(ZYCH) which is a promising therapeutic for liver fibrosis. 11(α)-Methoxysaikosaponin F has an IC50 of 387.7 nM with viability of hepatic stellate cells-T6 (HSCs-T6). Triterpenoid saponins have numerous targets, important network positions, and strong inhibitory activity .
|
-
- HY-15160A
-
|
Polo-like Kinase (PLK)
|
Cancer
|
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-139467
-
|
SHP2
PKC
|
Metabolic Disease
|
PF-04577806 is a potent, selective and ATP competitive PKC inhibitor. PF-04577806 shows potent inhibitory activity towards PKCα, PKCβI, PKCβII, PKCγ, and PKCθ with IC50s of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. PF-04577806 can reverse retinal vascular leakage in diabetic rats .
|
-
- HY-132842A
-
(S)-DZD9008
|
EGFR
Btk
|
Cancer
|
(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK .
|
-
- HY-144315
-
|
HDAC
|
Cancer
|
Snail/HDAC-IN-1 is a potent Snail/HDAC dual target inhibitor. Snail/HDAC-IN-1 displays potent inhibitory activity against HDAC1 with an IC50 of 0.405 μM and potent inhibition against Snail with a Kd of 0.18 μM. Snail/HDAC-IN-1 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis .
|
-
- HY-146335
-
|
CDK
|
Cancer
|
CLK1/4-IN-1 (compound 31) is a potent and selective Clk1 and Clk4 inhibitor with an IC50 value of 9.7 nM and 6.6 nM, respectively. CLK1/4-IN-1 has growth inhibitory activities against T24 cancer cells with GI50 of 1.1 μM. CLK1/4-IN-1 can be used for researching anticancer .
|
-
- HY-146462
-
|
Apoptosis
ROS Kinase
|
Cancer
|
Anticancer agent 59 (compound 11) has inhibitory activity against kinds of cancer cell lines, especially in A549 with IC50 of 0.2 μM. Anticancer agent 59 induces apoptosis and an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 59 significantly decreases mitochondrial membrane potential. Anticancer agent 59 can suppress tumor growth in A549 mouse xenograft model .
|
-
- HY-150958
-
|
RAD51
|
Cancer
|
RAD51-IN-8, a new RAD51 binder, is a RAD51-BRCA2 inhibitor that inhibits the RAD51 BRCA2 protein protein interaction. RAD51-IN-8 also is a protein−protein interaction (PPI) inhibitor. RAD51-IN-8 has inhibitory activity for H4A4 with an EC50 value of 19 μM .
|
-
- HY-152223
-
|
PCSK9
|
Cardiovascular Disease
|
PCSK9-IN-11 (compound 5r) is a potent and orally active PCSK9 inhibitor. PCSK9-IN-11 exhibits PCSK9 transcriptional inhibitory activity in HepG2 cells, with an IC50 of 5.7 μM. PCSK9-IN-11 increases LDL receptor (LDLR) protein level. PCSK9-IN-11 can be used for atherosclerosis research .
|
-
- HY-N0970
-
|
Others
|
Others
|
(4Z)-Lachnophyllum lactone is a enyne derivative. (4Z)-Lachnophyllum lactone shows growth inhibitory activity against Lemna paucicostata (IC50=104 μM), which is a problematic and invasive weed . (4Z)-Lachnophyllum lactone is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P5483
-
|
Bacterial
|
Others
|
Retro-indolicidin is a biological active peptide. (Reverse peptide of indolicidin (Rev4) is a 13-amino acid residue peptide based on the sequence of indolicidin. Indolicidin, a member of the cathelicidin protein family, is a 13-amino acid residue cationic, antimicrobial peptide-amide isolated from the cytoplasmic granules of bovine neutrophils. The synthetic peptide Rev4 has been shown to possess strong antimicrobial as well as protease inhibitory activities in vitro.)
|
-
- HY-N12161
-
|
Others
|
Metabolic Disease
|
3-Acetyl-11-keto-ursolic acid (Compound 18) is a triterpenoid compound derived from Eriobotrya japonicaleaves. 3-Acetyl-11-keto-ursolic acid has 11B-hydroxysteroid dehydrogenase 1 (11b-HSD1) inhibitory activity. 3-Acetyl-11-keto-ursolic acid can be used for anti-diabetes research .
|
-
- HY-N12198
-
|
Others
|
Cancer
|
Mollicellin H is a secondary metabolite of the fungus C. brasiliense and has a wide range of biological activities, including immunomodulation, cytotoxicity and anti-tumor effects. The growth inhibitory effects (GI50s) of Mollicellin H on human breast cancer (Bre04), human lung (Lu04) and human neuroma (N04) cell lines are 5.1 μg/mL, 6.5 μg/mL and 2.5 μg/mL respectively .
|
-
- HY-156181
-
|
Carbonic Anhydrase
|
Cancer
|
hCAIX/XII-IN-8 (compound 3g) is a potent human (carbonic anhydrase) CA IX and XII inhibitor, with Ki values of 8.5 and 6.7 nM, respectively. hCAIX/XII-IN-8 shows particularly strong inhibitory activity against the tumor-associated membrane-bound isoforms, hCA IX and XII, while maintaining a high selectivity ratio over cytosolic off-target isoforms hCA I and II .
|
-
- HY-162488
-
|
Fungal
|
Infection
|
Laccase-IN-3 (Compound 2b) is a laccase inhibitor (IC50 = 1.02= μM) with significant antifungal activity. Laccase-IN-3 shows superior inhibitory effect on Botryosphaeria dothidea (EC50 = 0.17 mg/L). Laccase-IN-3 effectively blocks the catalytic function of laccase by binding to its active center. Laccase-IN-3 also disrupts pathogen cell membrane integrity and increases ROS .
|
-
- HY-161569
-
|
YAP
|
Cancer
|
TEAD-IN-11 (compound 38) has a good inhibitory effect on TEAD1 (IC50=8.7 nM), TEAD2 (IC50=3.4 nM), TEAD3 (IC50=5.6 nnM). TEAD-IN-11 has good selective activity against TEAD1-3 as a covalent inhibitor. TEAD-IN-11 can be used for cancer research .
|
-
- HY-15306
-
SB-497115
|
Thrombopoietin Receptor
Bacterial
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
Eltrombopag (SB-497115) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag can be used for the research of cardiovascular. Eltrombopag also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag can induce apoptosis in hepatocellular carcinomab (HCC) as well .
|
-
- HY-N0057
-
3,4-Di-O-caffeoylquinic acid; Isochlorogenic acid B
|
Glucosidase
Influenza Virus
Apoptosis
Endogenous Metabolite
|
Infection
Cancer
|
3,4-Dicaffeoylquinic acid (3,4-Di-O-caffeoylquinic acid), naturally isolated from Laggera alata, has antioxidative, DNA protective, neuroprotective and hepatoprotective properties. 3,4-Dicaffeoylquinic acid exerts apoptosis-mediated cytotoxicity and α-glucosidase inhibitory effects. 3,4-Dicaffeoylquinic acid possesses a unique mechanism of anti-influenza viral activity, that is, enhancing viral clearance by increasing TRAIL .
|
-
- HY-N0619
-
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM .
|
-
- HY-19807
-
Indirubin-3'-oxime
|
GSK-3
CDK
Lipoxygenase
|
Cancer
|
Indirubin-3'-monoxime is a potent GSK-3β inhibitor, and weakly inhibits 5-Lipoxygenase, with IC50s of 22 nM and 7.8-10 µM, respectively; Indirubin-3'-monoxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, with IC50s of 100 and 180 nM.
|
-
- HY-121495
-
|
Parasite
|
Infection
|
BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC50 of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves .
|
-
- HY-N0241
-
|
Cholinesterase (ChE)
|
Metabolic Disease
|
Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM . Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL . Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM .
|
-
- HY-124618A
-
|
Flavivirus
Dengue virus
HCV
HIV
|
Infection
|
FGI-106 tetrahydrochloride is a potent and broad-spectrum inhibitor with inhibitory activity against multiple viruses. FGI-106 tetrahydrochloride is active against Ebola, Rift Valley and Dengue Fever viruses with EC50s of 100 nM, 800 nM and 400-900 nM, respectively. FGI-106 tetrahydrochloride also inhibits non-hemorrhagic fever viruses HCV and HIV-1 with EC50s of 200 nM and 150 nM, respectively .
|
-
- HY-146746
-
|
HIV
|
Infection
|
HIV-1 inhibitor-19 is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-19 maintains its inhibitory activity against L100I, K103N and V106A/ F227L mutant strains with EC50s of 7.3 nM, 9.2 nM and 21.0 nM, respectively[1].
|
-
- HY-144113
-
|
HIV
|
Infection
|
HIV-1 inhibitor-14 (compound 14b) is a highly potent and broad-spectrum HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor with an EC50 of 0.14 μM for HIV-1 RT. HIV-1 inhibitor-14 has inhibitory activity against HIV-1 WT and resistant strains with EC50s of 5.79 ~ 28.3 nM .
|
-
- HY-153103
-
|
LRRK2
JAK
AMPK
|
Inflammation/Immunology
|
LRRK2/NUAK1/TYK2-IN-1 (conpound 226) shows inhibitory activity toward LRRK2 (Wt), LRRK2 (G2019), TYK2 and NUAK1, with IC50 values lower than 10 nM. LRRK2/NUAK1/TYK2-IN-1 can be used for autoimmune disease research .
|
-
- HY-N1773
-
|
Others
|
Cancer
|
5,7,3' -tri-O-Methyl (-)-epicatechin (Compound 13) is a phospholipase Cγ1 (PLCγ1) inhibitor. 5,7,3' -tri-o-methyl (-)-epicatechin has a methylene dioxy benzene ring and can express inhibitory activity against PLCγ1. 5,7,3' -tri-O-Methyl (-)-epicatechin can be used in the study of chemotherapy and chemopexic agents for cancer .
|
-
- HY-N11957
-
|
Others
|
Inflammation/Immunology
|
Angeloylbinankadsurin A (compound 7) is an anti-rheumatoid arthritis (RA) agent that can be isolated from EtOAc and CH2Cl2 extracts of Black Tiger Beard. Angeloylbinankadsurin A exhibits inhibitory activity on RA-FLS cells (IC50=11.70 μM). Angeloylbinankadsurin A is slightly toxic to human cancer cell lines (Hela and BGC-823) (IC50=19.9 μM, 21.93 μM) .
|
-
- HY-158008
-
|
Ras
|
Cancer
|
(R)-G12Di-7 is a covalent ligand for KRAS-G12D, which selectively labels K-Ras-G12D·GDP and K-Ras-G12D·GppNHp. (R)-G12Di-7 exhibits inhibitory activity against G12D mutated cancer cells .
|
-
- HY-117005
-
|
Bacterial
|
Infection
|
C450-0730 is an antagonist targeting the AHL membrane-bound sensor kinase and is an antagonist of the nine-transmembrane protein LuxN of Vibrio harveyi . C450-0730 competitively binds to the LuxN AI-1 binding site and specifically antagonizes the LuxN/AI-1 quorum sensing signal in Vibrio harveyi. The inhibitory activity of C450-0730 against LuxN I209F was not significant .
|
-
- HY-18071
-
BI-9627
1 Publications Verification
|
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
BI-9627 is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
|
-
- HY-125182
-
|
HCV
|
Infection
|
SMCypI C31 is a non-peptidic cyclophilin inhibitor with potent peptidyl-prolyl cis/trans isomerases (PPIase) inhibitory activity (IC50 of 0.1 µM). SMCypI C31 shows pangenotype anti-HCV activity with EC50s ranging from 1.20 to 7.76 μM for genotype 1a, 1b, 2a, 3a, and 5a HCV subgenomic replicons (HCV-SGRs) and chimeric genotype 2a/4a HCV-SGRs. SMCypI C31 disrupts the cyclophilin A-NS5A interaction .
|
-
- HY-18071A
-
|
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
BI-9627 hydrochloride is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
|
-
- HY-N10439
-
|
Glucosidase
|
Inflammation/Immunology
|
3β-Acetoxy-hop-22(29)-ene (compound 1) is a potent anti-inflammatory agent. 3β-Acetoxy-hop-22(29)-ene shows high inhibitory activity of yeast α-glucosidase, with an IC50 of 5.74 μM. 3β-Acetoxy-hop-22(29)-ene inhibits MPO (myeloperoxidase) activity in a dose-dependent manner in mouse ear edema model induced by 12-O-tetradecanoylphorbol acetate (TPA), with an IC50 of 0.23 μmol/ear .
|
-
- HY-N10503
-
|
Tyrosinase
Ras
Raf
MAPKAPK2 (MK2)
Apoptosis
|
Cancer
|
Norartocarpetin is a tyrosinase inhibitor. Norartocarpetin has strong tyrosinase inhibitory activity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells .
|
-
- HY-109968A
-
CEP-26401 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
|
-
- HY-109968
-
CEP-26401
|
Histamine Receptor
|
Neurological Disease
|
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
|
-
- HY-149539
-
|
FLT3
RET
|
Cancer
|
PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po) .
|
-
- HY-152120
-
Aiphanol
|
COX
VEGFR
|
Inflammation/Immunology
Cancer
|
(±)-Aiphanol is a newly discovered stilbenolignan analog. (±)-Aiphanol exhibits significant anti-inflammatory activity, acting through inhibition of COX-1 and COX-2. The inhibitory effect on COX-1 (IC50 = 1.9 μM) is particularly strong, while the effect on COX-2 (IC50= 9.9 μM) is relatively weak .(±)-Aiphanol effectively inhibits VEGFR2 (IC50=0.92 µM). (±)-Aiphanol blocks angiogenesis and promotes apoptosis through inhibition of VEGFR2 and COX2 activity. (±)-Aiphanol is orally active .
|
-
- HY-10431
-
SB-431542
Maximum Cited Publications
169 Publications Verification
|
Organoid
TGF-β Receptor
Apoptosis
|
Cancer
|
SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways .
|
-
- HY-N0005
-
Diferuloylmethane; Natural Yellow 3; Turmeric yellow
|
Histone Acetyltransferase
Epigenetic Reader Domain
Keap1-Nrf2
Autophagy
Mitophagy
Influenza Virus
Ferroptosis
|
Cancer
|
Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
|
-
- HY-15306A
-
Eltrombopag diethanolamine salt; SB-497115GR
|
Thrombopoietin Receptor
Bacterial
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
Eltrombopag Olamine (Eltrombopag diethanolamine salt) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag Olamine owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag Olamine can be used for the research of cardiovascular. Eltrombopag Olamine also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag Olamine can induce apoptosis in hepatocellular carcinomab (HCC) as well .
|
-
- HY-N2025
-
|
PPAR
Glucosidase
|
Metabolic Disease
|
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
|
-
- HY-N1365
-
6-Hydroxy-7-methoxycoumarin
|
HBV
|
Infection
Cancer
|
Isoscopoletin (6-Hydroxy-7-methoxycoumarin) is an active constituent in Artemisia argyi leaves. Isoscopoletin shows substantial inhibition against cell proliferation, with IC50s of 4.0 μM and 1.6 μM for human CCRF-CEM leukaemia cells and multidrug resistant subline CEM/ADR5000, respectively . Isoscopoletin (6-Hydroxy-7-methoxycoumarin) possesses inhibitory activity against HBV replication .
|
-
- HY-N0396
-
|
COX
NO Synthase
|
Inflammation/Immunology
|
Harpagoside can be obtained by Harpagophytum procumbens, which has anti-inflammatory, anti-cancer, protective activity, and efficacy. Harpagoside has an inhibitory effect on COX-1 and COX-2 active, and suppresses NO production. Harpagoside inhibits HepG2 cell lipid polysaccharide, which is a protein that is expressed horizontally and selectively, and has anti-inflammatory and latent pain effects. Harpagoside has the ability to protect the body, and has a degenerative effect on the β-oxidation (Aβ).
|
-
- HY-19269
-
|
Elastase
|
Inflammation/Immunology
|
FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect .
|
-
- HY-131447
-
KY19382
1 Publications Verification
A3051
|
GSK-3
Wnt
β-catenin
|
Metabolic Disease
|
KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50s of 19 and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases .
|
-
- HY-15160C
-
|
Polo-like Kinase (PLK)
|
Cancer
|
TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-15306S
-
SB-497115-13C4
|
Thrombopoietin Receptor
Bacterial
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
Eltrombopag- 13C4 (SB-497115- 13C4) is 13 sup>C-labeled Z-Eltrombopag. Z-Eltrombopag is an orally active thrombopoietin-receptor non-peptide agonist with platelet-stimulating activity for the study of chronic immune thrombocytopenia. Eltrombopag also has strong inhibitory effects on multidrug-resistant Staphylococcus aureus (Staphylococcus aureus) and can induce apoptosis (apoptosis) in liver cancer cells .
|
-
- HY-143208
-
|
DNA/RNA Synthesis
|
Cancer
|
HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt has inhibitory activity against pre-miR-21 RNA. HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt has the potential for the research of neoplastic disease such as cancer and especially cancers expressing miR-21 (extracted from patent WO2021087084A1, compound 25) .
|
-
- HY-143743
-
|
Influenza Virus
|
Infection
|
Cap-dependent endonuclease-IN-2 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-2 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-2 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent WO2019052565A1, compound 28) .
|
-
- HY-143755
-
|
Influenza Virus
|
Infection
|
Cap-dependent endonuclease-IN-9 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-9 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-9 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent CN112521386A, compound VI-1) .
|
-
- HY-144039
-
|
DNA-PK
|
Cancer
|
DNA-PK-IN-6 is a potent inhibitor of DNA-PK. DNA-PK-IN-6 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-6 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of agent resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021197159A1, compound 6) .
|
-
- HY-144038
-
|
DNA-PK
|
Cancer
|
DNA-PK-IN-5 is a potent inhibitor of DNA-PK. DNA-PK-IN-5 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-5 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of agent resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021204111A1, compound 2) .
|
-
- HY-144306
-
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer .
|
-
- HY-118528A
-
|
TGF-β Receptor
|
Endocrinology
|
TP0427736 hydrochloride is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50=836 nM). TP0427736 hydrochloride also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. TP0427736 hydrochloride can be used for the research of androgenic alopecia (AGA) .
|
-
- HY-144636
-
|
Atg4
Cathepsin
Phospholipase
Autophagy
|
Cancer
|
Atg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer agents via autophagy inhibition .
|
-
- HY-144664
-
|
Bacterial
Thymidylate Synthase
|
Infection
|
MtTMPK-IN-2 (compound 15) is a potent Mycobacterium tuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 value of 1.1 μM. MtTMPK-IN-2 has inhibitory activity against Mtb H37Rv (MIC = 12.5 μM). MtTMPK-IN-2 exhibits certain cytotoxicity in human fibroblast cells MRC-5 (EC50 = 6.1 μM). MtTMPK-IN-2 can be used for researching tuberculosis .
|
-
- HY-144665
-
|
Bacterial
Thymidylate Synthase
|
Infection
|
MtTMPK-IN-3 (compound 25) is a potent Mycobacterium tuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 value of 0.12 μM. MtTMPK-IN-3 has inhibitory activity against Mtb H37Rv (MIC = 12.5 μM). MtTMPK-IN-3 exhibits certain cytotoxicity in human fibroblast cells MRC-5 (EC50 = 12.5 μM). MtTMPK-IN-3 can be used for researching tuberculosis .
|
-
- HY-146351
-
|
HDAC
|
Neurological Disease
|
HDAC-IN-38 (compound 13) is a potent HDAC inhibitor. HDAC-IN-38 shows similar micro-molar inhibitory activity toward HDAC1, 2, 3, 5, 6, and 8. HDAC-IN-38 increases cerebral blood flow (CBF), attenuates cognitive impairment, and improves hippocampal atrophy. HDAC-IN-38 also increases the level of histone acetylation (H3K14 or H4K5) .
|
-
- HY-147552
-
|
HIV
|
Infection
|
HIV-1 inhibitor-35 (compound 74) is a potent HIV-1 inhibitor with EC50s of 80 nM and 70 nM for LTR and CMV in HEK293 cells, respectively. HIV-1 inhibitor-35 has inhibitory activity against liver cancer cell HepG2 with a CC50 of 40 nM. HIV-1 inhibitor-35 can be used as HIV-1 latency reversing agent .
|
-
- HY-146678
-
|
HDAC
Amyloid-β
Cholinesterase (ChE)
|
Neurological Disease
|
HDAC6-IN-5 (compound 11b) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-5 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-5 can enhance neurite outgrowth without significant neurotoxicity .
|
-
- HY-146679
-
|
HDAC
Amyloid-β
Cholinesterase (ChE)
|
Neurological Disease
|
HDAC6-IN-6 (compound 6a) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-6 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-6 can enhance neurite outgrowth without significant neurotoxicity .
|
-
- HY-147851
-
|
Beta-secretase
|
Neurological Disease
|
BACE1-IN-12 (compound 7g) is a potent and BBB-penetrated BACE1 inhibitor, with an IC50 of 8.9 µM. BACE1-IN-12 shows selective BuChE (butyrylcholinesterase) inhibitory activity with an IC50 of 3.2 µM. BACE1-IN-12 shows effective antioxidant effect with an IC50 of 10.2 μM (DPPH). BACE1-IN-12 might be served as a potential anti-Alzheimer agent .
|
-
- HY-147992
-
|
EGFR
|
Cancer
|
EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research .
|
-
- HY-147994
-
|
EGFR
|
Cancer
|
EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research .
|
-
- HY-151374
-
|
PKD
|
Cancer
|
3-IN-PP1 is a protein kinase D (PKD) inhibitor. 3-IN-PP1 has potent pan-PKD inhibitory activity for PKD1, PKD2 and PKD3 with IC50 values of 108, 94 and 108 nM, respectively. 3-IN-PP1 also is a broad spectrum anticancer agent and has inhibition of several tumor cells growth. 3-IN-PP1 can be used for the research of cancer .
|
-
- HY-151534
-
|
Epigenetic Reader Domain
|
Cancer
|
PBRM1-BD2-IN-7 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-7 has inhibitory activity for PBRM1-BD2 with an IC50 value of 0.29 μM. PBRM1-BD2-IN-7 can be used for the research of cancer .
|
-
- HY-152030
-
|
Microtubule/Tubulin
MMP
Apoptosis
|
Cancer
|
Tubulin/MMP-IN-2 is dual inhibitor of tubulin and matrix metalloproteinases. Tubulin/MMP-IN-2 can strongly inhibit tubulin polymerization and induces cell apoptosis. Tubulin/MMP-IN-2 has inhibitory activities against MMP-2, MMP-3 and MMP-9 with IC50 values of 24.95 μM, 31.60 μM and 22.37 μM, respectively. Tubulin/MMP-IN-2 can be used for the research of cancer .
|
-
- HY-P4641
-
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
H-Trp-Phe-OH is a dipeptide consisting of tryptophan and phenylalanine (Trp-Phe). H-Trp-Phe-OH is also an antihypertensive peptide with inhibitory activity on angiotensin-converting enzyme (ACE), dose-dependently increases NO levels, and decreases endothelin-1 (ET-1) levels. H-Trp-Phe-OH (2 mg/kg; subcutaneous injection; 6 injections over 3 days) causes an increase in ovarian weight in female mice .
|
-
- HY-N1783
-
|
Phosphatase
|
Cancer
|
(24E)-3,4-Secocucurbita-4,24-diene-3,26,29-trioic acid is a potent PTP1B inhibitor, with an IC50 of 0.4 μM. (24E)-3,4-Secocucurbita-4,24-diene-3,26,29-trioic acid exhibits potent PTP1B inhibitory activity without cytotoxicity .
|
-
- HY-P2302
-
|
Antibiotic
Bacterial
Fungal
|
Infection
|
Defensin HNP-3 human is a cytotoxic antibiotic peptide known as "defensin". Defensin HNP-3 human has inhibitory activity against Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. Defensin HNP-3 human is initially synthesized as the 94 amino acids preproHNP(1-94), which is hydrolyzed to proHNP(20-94) and converted to mature HNP(65-94) after the removal of anion precursors .
|
-
- HY-155751
-
-
- HY-106961A
-
(Z)-ONO-AP 500-02
|
Others
|
Cardiovascular Disease
|
(Z)-ONO 1301 is the isomer of ONO 1301 (HY-106961), and can be used as an experimental control. ONO 1301 (ONO-AP 500-02), a prostaglandin (PG) I2 mimetic, is an orally active, long-acting prostacyclin agonist with thromboxane-synthase inhibitory activity. ONO 1301 promotes production of hepatocyte growth factor (HGF) from various cell types and ameliorates ischemia-induced left ventricle dysfunction in the mouse, rat and pig .
|
-
- HY-156103
-
|
Huntingtin
|
Neurological Disease
|
mHTT-IN-2 (compound 27) is a potent inhibitor (EC50=0.066 μM) of mutant huntingtin (mHTT). mHTT-IN-2 reduces canonical splicing of HTT RNA exons [49-50] and is a splicing regulator of the huntingtin (HTT) gene. mHTT-IN-2 exhibits inhibitory activity in vitro and in vivo in human HD stem cells and mouse BACHD models. mHTT-IN-2 may be used in the study of branaplam-related peripheral neuropathy .
|
-
- HY-149578
-
|
Microtubule/Tubulin
HDAC
|
Cancer
|
Tubulin/HDAC-IN-3 (compound 12a) is a potent tubulin/HDAC dual inhibitor. Tubulin/HDAC-IN-3 effectively disrupts tubulin polymerization (IC50: 5.4 μM). Tubulin/HDAC-IN-3 exhibits potent HDAC1/8 inhibitory activities, with IC50 values of 0.155 and 0.177 μM, respectively. Tubulin/HDAC-IN-3 works through blocking cellular cycle, inducing apoptosis and inhibiting colony formation .
|
-
- HY-14205
-
|
Monoamine Oxidase
|
Neurological Disease
|
NW-1772 (methanesulfonate) (22b) is a potent and selective monoamine oxidase (MAO) B inhibitor. NW-1772 (methanesulfonate) is the equivalent of HY-111156 NW-1772. NW-1772 has some advantages, such as rapid blood-brain barrier penetration, short-acting and reversible inhibitory activity, slight inhibition of selected cytochrome P450s, and low in vitro toxicity. NW-1772 can be used for the research of neurodegenerative diseases .
|
-
- HY-N0041R
-
Gypenoside IV (Standard)
|
NF-κB
COX
NO Synthase
|
Inflammation/Immunology
Cancer
|
Ginsenoside Rb3 (Standard) is the analytical standard of Ginsenoside Rb3. This product is intended for research and analytical applications. Ginsenoside Rb3 is extracted from steamed Panax ginseng C. A. Meyer. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
|
-
- HY-D2204
-
|
Phosphatase
Fluorescent Dye
|
Cancer
|
SHP1-IN-1 (compound 5p) is a fluorescent probe for the protein tyrosine phosphatase SHP1 containing the Src homology 2 domain. SHP1-IN-1 has SHP1 inhibitory activity, selectivity for Fe 3+ ions and good fluorescence properties. SHP1-IN-1 exhibits aggregation post-quenching (ACQ) effect, good interference immunity and low detection limit (5.55 μM) .
|
-
- HY-N12606
-
|
Fungal
|
Infection
|
Neodidymelliosides A (compound 1)It is a secondary metabolite of fungi and has a significant inhibitory effect on Staphylococcus aureus and Candida albicans biofilms. Neodidymelliosides AIt also has anti-cancer activity and can inhibit KB3.1 (cervix),PC-3 (prostate),MCF-7(breast),SKOV-3 (ovary),A431 (skin )and A549 (lung )Cell viability of cell lines .
|
-
- HY-163343
-
|
Phosphodiesterase (PDE)
STING
|
Cancer
|
Enpp-1-IN-20 (Compound 31) is an ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) inhibitor, with an IC50 of 0.09 nM. Enpp-1-IN-20 has strongest inhibitory activity in the cell-based assay, with an IC50 of 8.8 nM. Enpp-1-IN-20 has significant potency in both ENPP1 inhibition and STING pathway stimulation in vitro. Enpp-1-IN-20 can be used for the research of cancer .
|
-
- HY-163453
-
|
EGFR
|
Cancer
|
HER2-IN-19 (Compound 10e) is a potent inhibitor of HER2 and EGFR with IC50 values of 0.87 respectively and 3.5 nM. HER2-IN-19 has potent inhibitory activity against tumor cells, IC50 NCI-N87 = 1.63 nM, IC50 BT474= 15.17 nM, IC50 BaF3-HER2YVMA = 1.49 nM .
|
-
- HY-158365
-
|
LRRK2
|
Neurological Disease
|
LRRK2-IN-14 (Compound 8) is an orally active LRRK2 inhibitor. LRRK2-IN-14 has an IC50 of 6.3 nM for LRRK2(G2019S) cell activity.LRRK2-IN-14 has an inhibitory effect on hERG (IC50=22 μM). LRRK2-IN-14 has blood-brain barrier permeability .
|
-
- HY-101664R
-
|
Proton Pump
TOPK
|
Inflammation/Immunology
Cancer
|
Ilaprazole (Standard) is the analytical standard of Ilaprazole. This product is intended for research and analytical applications. Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-136358
-
|
Ephrin Receptor
|
Neurological Disease
Cancer
|
LDN-211904 is an inhibitor of EphB3 receptor tyrosine kinase. LDN-211904 enhances the inhibitory activity of EphB3 kinase by maintaining the 2-chloroaniline group and introducing a phenyl or small electron donor substituent to the 5 position of pyrazole and [1,5-a] pyridine. LDN-211904 can be used as a molecular probe to study the function and signaling pathways of EphB3 receptors, especially in the nervous system during neurodevelopment and adulthood .
|
-
- HY-160831
-
PQQ-TME
|
Others
|
Neurological Disease
|
PQQ-trimethylester (PQQ-TME) is a synthetic compound that is a trimethylester derivative of pyrroloquinoline quinone (PQQ). PQQ-trimethylester has twice the blood-brain barrier permeability of PQQ (HY-100196) in vitro. In addition, PQQ-trimethylester shows strong inhibitory activity against α-synuclein, amyloid β1-42 (Aβ1-42) and prion protein fibrillation. PQQ-trimethylester can be used in the study of neurodegenerative diseases .
|
-
- HY-103019E
-
BAY-1251152; VIP152
|
Others
|
Others
|
Enitociclib (VIP152; BAY-1251152) is a selective CDK9 inhibitor. Known for its unique benzyl sulfoxide moiety, VIP152 has demonstrated promising efficacy and tolerability both in vitro and in vivo, including in mouse and rat xenograft models via weekly intravenous infusions Highly effective and well tolerated. VIP152 shows promising long-term single-agent inhibitory activity against double-click refractory diffuse large B-cell lymphoma .
|
-
- HY-12403
-
TXA127; Angiotensin (1-7); Ang-(1-7)
|
Angiotensin Receptor
Angiotensin-converting Enzyme (ACE)
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
|
Angiotensin 1-7 (Ang-(1-7)) is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 inhibits purified canine ACE activity (IC50=0.65 μM). Angiotensin 1-7 acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium. Angiotensin 1-7 shows anti-inflammatory activity .
|
-
- HY-100513A
-
|
Apoptosis
DNA/RNA Synthesis
Antibiotic
|
Cancer
|
Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM) . Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis . Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo .
|
-
- HY-12403A
-
TXA127 acetate; Angiotensin (1-7) (acetate); Ang-(1-7) (acetate)
|
Angiotensin Receptor
Angiotensin-converting Enzyme (ACE)
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
|
Angiotensin 1-7 (Ang-(1-7)) acetate is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 acetate inhibits purified canine ACE activity (IC50=0.65 μM). Angiotensin 1-7 acetate acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 acetate blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium .
|
-
- HY-154855
-
|
HDAC
|
Cancer
|
HDAC-IN-56 ((S)-17b) is an orally active class I histone deacetylase (HDAC) inhibitor with IC50 values of 56.0 ± 6.0, 90.0 ± 5.9, 422.2 ± 105.1, >10000 nM for HDAC1, HDAC2, HDAC3, and HDAC4-11, respectively. HDAC-IN-56 has potent inhibitory activity while strongly increasing intracellular levels of acetylhistone H3 and P21 and effectively inducing G1 cell cycle arrest and apoptosis.HDAC-IN-56 has antitumor activity .
|
-
- HY-158327
-
|
Others
|
Others
|
Insecticidal agent 9 (Compound I-17) is an insecticide with good insecticidal activity. Insecticidal agent 9 has LC50 values of 93.32 mg/L and 114.79 mg/L against Plutella xylostella and Ostrinia furnacalis respectively, and exhibits a mortality rate of up to 86.1% against Spodoptera frugiperda at a concentration of 500 mg/L. Insecticidal agent 9 can act simultaneously on the ecdysone receptor (EcR) and three chitinases (OfChtI, OfChtII, and OfChi-h), demonstrating good binding activity (to EcR) and inhibitory rates (to the three chitinases). Insecticidal agent 9 can be used in research for pest management .
|
-
- HY-B1138R
-
|
COX
Caspase
|
Inflammation/Immunology
|
Fenbufen (Standard) is the analytical standard of Fenbufen. This product is intended for research and analytical applications. Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor .
|
-
- HY-16986
-
|
Histone Methyltransferase
|
Cancer
|
EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers . EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-10943
-
GNF-7
2 Publications Verification
|
Bcr-Abl
Ack1
|
Cancer
|
GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-Abl WT and Bcr-Abl T315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies .
|
-
- HY-103160A
-
|
Adenosine Deaminase
Phosphodiesterase (PDE)
Influenza Virus
|
Infection
Cardiovascular Disease
Neurological Disease
Cancer
|
EHNA hydrochloride is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA hydrochloride exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA hydrochloride play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects .
|
-
- HY-N0619A
-
Mulberroside D
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory and anti-apoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM .
|
-
- HY-N0930B
-
|
AMPK
Bacterial
|
Infection
Metabolic Disease
|
Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains .
|
-
- HY-146005
-
|
Microtubule/Tubulin
|
Neurological Disease
Inflammation/Immunology
|
Tau-aggregation and neuroinflammation-IN-1 is a potent tau-aggregation and neuroinflammation inhibitor. Tau-aggregation and neuroinflammation-IN-1 exhibits remarkable inhibitory activities against AcPHF6 and full-length tau aggregation. Tau-aggregation and neuroinflammation-IN-1 has a low cytotoxicity and reduced NO release in LPS-stimulated BV2 cells. Tau-aggregation and neuroinflammation-IN-1 can reverse okadaic acid-induced memory impairment in rats .
|
-
- HY-146000
-
|
Influenza Virus
|
Inflammation/Immunology
|
Influenza virus-IN-3 (compound 9) is a potent and selective influenza virus inhibitor with IC50s of 0.88, 0.10, 5.5, 0.51 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-3 shows antiviral and NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-3 shows low cytotoxicity with an CC50 of >200 µM .
|
-
- HY-146302
-
|
Apoptosis
|
Cancer
|
14-3-3η Protein inhibitor 1 (Compound C11) is a 14-3-3η protein inhibitor with a KD of 35 µM. 14-3-3η Protein inhibitor 1 shows inhibitory activities against several typical human liver cancer cell lines. 14-3-3η Protein inhibitor 1 induces cell apoptosis and G1-S cell cycle arrest with good metabolic stability .
|
-
- HY-124623
-
|
Parasite
|
Infection
|
DNDI-8219 (compound 58) is a potent selective and orally active trypanocidal agent, possessing inhibitory activity against Trypanosoma cruzi (T. cruzi) with an IC50 of 0.4 μM. DNDI-8219 has low cytotoxicity (L6 cells IC50 > 100 μM). DNDI-8219 can effectively cure chronic T. cruzi infection and markedly reduce parasite burdens in mouse model. DNDI-8219 has good solubility, metabolic stability and safety.
|
-
- HY-151528
-
|
Epigenetic Reader Domain
|
Cancer
|
PBRM1-BD2-IN-1 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-1 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 0.7 μM and 0.2 μM, respectively. PBRM1-BD2-IN-1 can be used for the research of cancer .
|
-
- HY-151529
-
|
Epigenetic Reader Domain
|
Cancer
|
PBRM1-BD2-IN-2 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-2 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. PBRM1-BD2-IN-2 can be used for the research of cancer .
|
-
- HY-152005
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2 3CLpro-IN-6 is a reversible covalent inhibitor of SARS-CoV-2 3CL protease. SARS-CoV-2 3CLpro-IN-6 has potent inhibitory activity for SARS-CoV-2 3CL pro with an IC50 value of 4.9 μM. SARS-CoV-2 3CLpro-IN-6 can be used for the research of coronavirus disease 2019 (COVID-19) .
|
-
- HY-N10868
-
|
LIM Kinase (LIMK)
|
Cancer
|
8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide (compound 3), a sesquiterpene, has anti-LIMK1 activity. 8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide has inhibitory property on cell motility .
|
-
- HY-N3364
-
|
Flavivirus
Dengue virus
TNF Receptor
NF-κB
NO Synthase
COX
JNK
p38 MAPK
IKK
|
Infection
Inflammation/Immunology
|
Lucidone, an anti-inflammatory agent that can be isolated from the fruit of Lindera erythrocarpa Makino. Lucidone inhibits LPS-induced NO and PGE2 production in RAW 264.7 mouse macrophages. Lucidone also decreases TNF-α secretion, iNOS and COX-2 expression. Lucidone prevents NF-κB translocation and inhibits JNK and p38MAPK signals. Lucidone also has inhibitory activity against Dengue virus (DENV) (EC50=25 μM) .
|
-
- HY-155198
-
|
Fungal
|
Infection
|
Antifungal agent 72 (Compound B8) is a potent antifungal agent. Antifungal agent 72 suppresses the function of efflux pump and down-regulates the resistance-associated genes through blocking the Pdr1-KIX interaction (Ki: 11.7 μM). Antifungal agent 72 is active against Fluconazole (HY-B0101)-resistant with a MIC value of 63 ng/mL, and shows synergistic inhibitory activity with Fluconazole. Antifungal agent 72 can be used for C. glabrata infection research .
|
-
- HY-125085
-
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
ALDH3A1-IN-3 (CB29) is a selective inhibitor of ALDH3A1, with a Ki value of 4.7 μM and an IC50 value of 16 μM. ALDH3A1-IN-3 has no inhibitory potential on the in vitro activity of ALDH1A1, ALDH1A2, ALDH1A3, ALDH1B1, or ALDH2. ALDH3A1-IN-3 can be used in cellular oxidation and cancer research .
|
-
- HY-B1138S
-
|
Isotope-Labeled Compounds
COX
Caspase
|
Inflammation/Immunology
|
Fenbufen-d9 (CL-82204-d9) is the deuterium labeled Fenbufen. Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor[1][2][3][4][5].
|
-
- HY-124346
-
|
Others
|
Metabolic Disease
|
T-3364366 is a reversible, slow-binding, thienopyrimidinone delta-5 desaturase (D5D) inhibitor with IC50s of 1.9 nM and 2.1 nM in HepG2 and RLN-10 cells, respectively. T-3364366 exhibits potent D5D (IC500=19 nM) inhibitory activity and excellent selectivity away from delta-6 desaturase (D6D, IC50=6200 nM) and delta-9 desaturase (stearoyl-CoA desaturase, SCD,50 >10000 nM) in the enzymatic activity assay .
|
-
- HY-149008
-
|
Amylases
|
Metabolic Disease
Cancer
|
α-Amylase-IN-3 (Compound 4) is a none-competitive type of α-Amylase inhibitor with an IC50 value of 18.04 μM, which also has radical scavenging activities (DPPH and ABTS) with IC50 values of 16.04 μM (DPPH) and 16.99 μM (ABTS), respectively. α-Amylase-IN-3 has good protein–ligand interactions profile against α-Amylase. α-Amylase-IN-3 may have pharmacological activities such as anti-oxidative, anti-inflammatory inhibitory, which is helpful for the development of diabetes and oxidative stress associated disease .
|
-
- HY-155007
-
|
Bacterial
|
Infection
|
DNA gyrase B-IN-2 (Compound E) is a 2-aminobenzothiazole-based DNA gyrase B inhibitor with promising activity against ESKAPE bacterial pathogens. DNA gyrase B-IN-2 showed low nanomolar inhibition of DNA gyrase (IC50 < 10 nM) and broad-spectrum antibacterial activity against pathogens belonging to the ESKAPE group, with the minimum inhibitory concentration < 0.03 μg/mL for most Gram-positive strains and 4–16 μg/mL against Gram-negative E. coli, Acinetobacter baumannii, Pseudomonas aeruginosa, and Klebsiella pneumoniae.DNA gyrase B-IN-2 can be used for the research of infection .
|
-
- HY-15730
-
HM781-36B; NOV120101
|
EGFR
Apoptosis
|
Cancer
|
Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFR wt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFR T790M and EGFR L858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity .
|
-
- HY-16986A
-
|
Histone Methyltransferase
|
Cancer
|
EPZ-011989 trifluoroacetate is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers . EPZ011989 (trifluoroacetate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-N0568
-
Asiaticoside A
|
Endogenous Metabolite
Apoptosis
Autophagy
Keap1-Nrf2
p38 MAPK
Caspase
|
Cardiovascular Disease
Others
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
|
Madecassoside is a pentacyclic triterpene isolated from Centella asiatica and has anti-inflammatory properties. Antioxidant and anti-aging effects.
Madecassoside is a pentacyclic triterpene isolated from Centella asiatica. Madecassoside is orally active and has inhibitory properties against inflammation, oxidation, apoptosis and autophagy. Madecassosid inhibits activities of p38 MAPK and NF-kB [5][6], exhibits an anti-apopototic property, activates Nrf2 expression to reduce the neurotoxicity . Madecassoside can be used in endocrine diseases, cardiovascular diseases, skin diseases and other diseases.
|
-
- HY-12214A
-
|
CDK
Apoptosis
|
Cancer
|
NVP-2 is a potent and selective ATP-competitive cyclin dependent kinase 9 (CDK9) probe, inhibits CDK9/CycT activity with an IC50 of 0.514 nM. NVP-2 displays inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases with IC50 values of 0.584 µM, 0.706 µM, and 0.605 µM, respectively. NVP-2 induces cell apoptosis.
|
-
- HY-14850
-
Netazepide; YF 476; YM-220
|
Cholecystokinin Receptor
|
Metabolic Disease
Endocrinology
|
Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC50 of 502 nM . Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with Ki values of 0.068, 0.62 and 0.19 nM, respectively .
|
-
- HY-111932
-
|
CDK
GSK-3
|
Cancer
|
Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively . Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β .
|
-
- HY-103444
-
|
MMP
|
Cancer
|
ARP-100 is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with S1' pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitory activity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM) .
|
-
- HY-12843
-
|
CDK
ERK
|
Cancer
|
Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities .
|
-
- HY-B1890
-
rel-Cianidanol; rel-Catechuic acid
|
COX
|
Infection
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
(±)-Catechin (rel-Cianidanol) This is a green tea polyester. Catechin possesses anti-cancer activity, which has led to its demise. (±)-Catechin 具有两种forms (+)-Catechin and its reflection body (-)-Catechin. (+)-Catechin inhibitory environment-1 (COX-1) IC50 为 1.4 μM. (-)-Catechin has the effect of promoting hBM-MSC adipose cell differentiation, increasing adipose tissue, and PPARγ horizontal. (±)-Catechin has anti-diabetic, anti-hypertrophic, anti-diabetic, anti-cardiovascular, anti-infective, and liver-protecting effects.
|
-
- HY-115973
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
AChE-IN-11 (compound 5C) is a triple inhibitor targeting AChE/MAO-B/BACE1 (IC50=7.9 μM, 9.9 μM, 8.3 μM, respectively) and a selective metal ion chelators. AChE-IN-11 exhibits mixed AChE inhibitory effects, binding to both CAS and PAS of AChE. AChE-IN-11 also exhibits good antioxidant activity (ORAC=2.5 eq) and potential neuroprotective effects in Alzheimer's disease .
|
-
- HY-146755
-
|
Trk Receptor
|
Cancer
|
TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA G595R, TRKA G667C, TRKA F589L, TRKC G623R, TRKC G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model .
|
-
- HY-146202
-
|
Phosphodiesterase (PDE)
|
Others
|
5-HT1A/5-HT7 receptor antagonist (5-HT1A Ki = 8 nM, Kb = 0.04 nM; 5-HT7 Ki = 451 nM, Kb = 460 nM) with PDE4B/PDE7A inhibitory activity (PDE4B IC50 = 80.4 μM; PDE7A IC50 = 151.3 μM) , its antidepressant like effect is stronger than that of escitalopram as a reference agent.
|
-
- HY-151153
-
|
HDAC
Microtubule/Tubulin
Caspase
Apoptosis
|
Cancer
|
HDAC1-IN-5 is a potent HDAC1 inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice .
|
-
- HY-148260
-
|
Ras
|
Cancer
|
KRAS G12D inhibitor 16 is a KRAS G12D inhibitor. KRAS G12D inhibitor 16 has inhibitory activity against KRAS G12D and KRAS G12D mutation with IC50 value of 0.7 nM and 0.35 μM, respectively. KRAS G12D inhibitor 16 can be used for the research of many malignant tumor, such as pancreatic ductal adenocarcinomas (PDAC), colon and rectal carcinomas (CRC), non-small cell lung carcinomas (NSCLC) .
|
-
- HY-149340
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
PD07 is an orally active AChE inhibitor (IC50: 0.29 μM for hAChE). PD07 also inhibits ChEs, BACE1 (IC50: 13.42 μM), and Aβ1–42 aggregation in in vitro. PD07 is an antioxidant, and shows DPPH inhibitory activity (IC50: 26.46 μM). PD07 improves memory and cognition in Scopolamine (HY-N0296)-induced amnesia rats. PD07 can be used for research of Alzheimer’s disease .
|
-
- HY-149555
-
|
Eukaryotic Initiation Factor (eIF)
|
Neurological Disease
|
DNL343 is a brain-penetrating activator of eukaryotic initiation factor 2B (eIF2B) that inhibits the abnormal integrated stress response (ISR). DNL343 inhibits ISR activity in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 has inhibitory potential in studies of vanishing white matter disease (VWMD) driven by eIF2B LOF and chronic ISR activation .
|
-
- HY-157966
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2 3CLpro-IN-23 (Compound Cd3) is a compound that can be isolated from Citrus depressa. SARS-CoV-2 3CLpro-IN-23 has good inhibitory activity to the SARS-CoV-2 spike protein, with KD of 0.79 μM. SARS-CoV-2 3CLpro-IN-23 can bind to key amino acid residue, disrupting the formation of the spike protein and h-ACE2 complex .
|
-
- HY-158106
-
|
CDK
|
Cancer
|
AZD8421 is a selective CDK2 inhibitor (IC50: 9 nM) with selectivity for CDK1, CDK4 and CDK6. AZD8421 inhibits cancer cell proliferation by inhibiting pRB phosphorylation, inducing cell cycle arrest and senescence. AZD8421 demonstrated promising single efficacy and synergy with CDK4/6 inhibitors such as Palbociclib (HY-50767) in in vivo breast and ovarian models. AZD8421 also has potent single-agent inhibitory activity against drug-resistant breast cancer cells.
|
-
- HY-15306R
-
|
Thrombopoietin Receptor
Bacterial
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
Eltrombopag (Standard) is the analytical standard of Eltrombopag. This product is intended for research and analytical applications. Eltrombopag (SB-497115) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag can be used for the research of cardiovascular. Eltrombopag also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag can induce apoptosis in hepatocellular carcinomab (HCC) as well .
|
-
- HY-P10281
-
|
Bacterial
|
Infection
|
RW3 is a small cationic hexapeptide with amphiphilic properties. RW3 targets the plasma membrane of bacteria and works by inhibiting cell respiration and cell wall synthesis. RW3 shows high biological activity against gram-positive bacteria and does not show significant cytotoxic or hemolytic effects in previous studies. RW3 quickly kills 97% of the initial colony forming units (CFU) within 10 minutes at twice the minimum inhibitory concentration (MIC). RW3 can be used in antimicrobial and antifungal studies .
|
-
- HY-13588A
-
SCE-129
|
Others
|
Others
|
Cefsulodin (SCE-129) showed potent activity against Pseudomonas aeruginosa and strains susceptible to penicillin and gentamicin, with effectiveness comparable to that of gentamicin and debendazole. However, its effectiveness was diminished against penicillin-resistant strains of P. aeruginosa, particularly strains that were also resistant to gentamicin. For P. aeruginosa maltofila, SCE-129 showed similar minimum inhibitory concentrations to penicillin, gentamicin, and debendazole. Pseudomonas cepacia strains generally showed moderate resistance to SCE-129 and penicillin, and high resistance to gentamicin and debendazole .
|
-
- HY-14863
-
CTA-018
|
VD/VDR
Cytochrome P450
|
Others
Endocrinology
|
Lunacalcipol (CTA-018), as a vitamin D analogue, has a dual role in the pathogenesis of Chronic Kidney Disease (CKD), as an agonist of vitamin D receptor and an antagonist of cytochrome P450 enzyme 24-hydroxylase. Lunacalcipol binds to VDR and regulates transcriptional activity of VDR by influencing ligand binding affinity, ligand-dependent coactivator recruitment or inhibitory factor dissociation, efficiency of ligand entry into target cells, tissue specificity and different metabolism of ligand. Lunacalcipol can be used in the study of CKD, especially Secondary Hyperparathyroidism (sHPT) .
|
-
- HY-B2097
-
YM 175; Bisphonal
|
Farnesyl Transferase
|
Metabolic Disease
|
Incadronate disodium (YM 175) is a bisphosphonate with strong inhibitory activity on bone resorption. Incadronate disodium indirectly stimulates renal 25-hydroxyvitamin D-1-hydroxylase by increasing circulating parathyroid hormone. Incadronate disodium, a cholesterol-lowering agent, is a potent inhibitor of rat liver microsomal squalene synthase (Ki=57 nM). Incadronate disodium inhibits sterol biosynthesis in mouse macrophage J774 cells (IC50=64 μM). Incadronate disodium has the potential for malignant tumors research .
|
-
- HY-N12964
-
|
Others
|
Others
|
4-Hydroxycanthin-6-one is a novel quinoline alkaloid isolated from the stem bark of the tree Ailanthus altissima. Five other known compounds were also found in the study. The structures of the new compounds were determined by interpretation of physical and spectroscopic data, and their absolute configurations were determined by electronic circular dichroism spectroscopy and quantum chemical calculations. These compounds showed significant inhibitory activity against lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells, showing potential anti-inflammatory properties .
|
-
- HY-139604
-
|
Apoptosis
|
Cancer
|
PCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) inhibitor with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability .
|
-
- HY-18540
-
|
MAGL
|
Metabolic Disease
Inflammation/Immunology
|
KT109 is a potent and an isoform-selective inhibitor of diacylglycerol lipase-β (DAGLβ) with an IC50 of 42 nM. KT109 has ~60-fold selectivity for DAGLβ over DAGLα. KT109 shows inhibitory activity against PLA2G7 (IC50=1 µM). KT109 shows negligible activity against FAAH, MGLL, ABHD11, and cytosolic phospholipase A2 (cPLA2 or PLA2G4A). KT109 perturbs a lipid network involved in macrophage inflammatory responses and lowers 2-arachidonoylglycerol (2-AG), arachidonic acid and eicosanoids in mouse peritoneal macrophages .
|
-
- HY-156470
-
|
Trk Receptor
Anaplastic lymphoma kinase (ALK)
c-Kit
EGFR
Pim
Casein Kinase
Checkpoint Kinase (Chk)
CDK
Apoptosis
|
Cancer
|
Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect .
|
-
- HY-161512
-
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
hAChE/hBACE-1-IN-4 (compound AK-2) is a quinazoline derivative. hAChE/hBACE-1-IN-4 shows significant inhibitory activity against hAChE and hBACE-1 enzymes (hAChE, IC50=0.283 μM; hBACE-1, IC50=0.231 μM). hAChE/hBACE-1-IN-4 has the potential to inhibit Aβ aggregation. hAChE/hBACE-1-IN-4 has non-neurotoxicity , blood-brain barrier permeability and oral activity. hAChE/hBACE-1-IN-4 can be used in Alzheimer's disease research .
|
-
- HY-N0058
-
Isochlorogenic acid C
|
HBV
Endogenous Metabolite
Apoptosis
Glucosidase
|
Infection
|
4,5-Dicaffeoylquinic acid (Isochlorogenic acid C) is an antioxidant, can be isolated from Gynura divaricata and Laggera alata. 4,5-Dicaffeoylquinic acid reduces islet cell apoptosis and improves pancreatic function in type 2 diabetic mice, and has obvious inhibitory activities against yeast α-glucosidase. 4,5-Dicaffeoylquinic acid inhibits prostate cancer cells through cell cycle arrest. 4,5-Dicaffeoylquinic acid also has anti-apoptotic, anti-injury and anti-hepatitis B virus effects .
|
-
- HY-126257
-
|
Akt
Apoptosis
|
Cancer
|
AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells .
|
-
- HY-129453
-
|
Integrin
|
Inflammation/Immunology
|
BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins .
|
-
- HY-144122
-
|
HIV
|
Infection
|
HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability .
|
-
- HY-147793
-
|
FGFR
|
Cancer
|
FGFR4-IN-12 (Compound A34) is a potent inhibitor of FGFR4. FGFR4-IN-12 exhibits improved FGFR4 inhibitory capability and selectivity and excellent anti-proliferative activities against FGFR4-dependent HCC cell lines. FGFR4-IN-12 has the potential for the research of cancer diseases . FGFR4-IN-12 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-147972
-
|
NF-κB
p38 MAPK
NO Synthase
COX
|
Inflammation/Immunology
|
NF-κB/MAPK-IN-1 (compound 11a) is a potent inhibitor of NF-κB and MAPK pathway. NF-κB/MAPK-IN-1 shows inhibitory activity against NO production, with an IC50 of 6.96 µM. NF-κB/MAPK-IN-1 suppresses LPS-induced iNOS, COX-2, ERΚ and P38 signaling activation. NF-κB/MAPK-IN-1 can prevent LPS induced inflammatory response in macrophages. NF-κB/MAPK-IN-1 can be used for rheumatoid arthritis (RA) research .
|
-
- HY-151928
-
|
JNK
|
Neurological Disease
|
JNK3 inhibitor-3 (compound 15g) is a selective, BBB permeable and orally active c-Jun N-terminal kinase 3 (JNK3) inhibitor. JNK3 inhibitor-3 has inhibitory activities to JNK1, JNK2 and JNK3 with IC50 values of 147.8, 44.0 and 4.1 nM, respectively. JNK3 inhibitor-3 significantly improves the memory in mouse dementia model. JNK3 inhibitor-3 can be used for the research of Alzheimer’s disease .
|
-
- HY-149295
-
|
PROTACs
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
PROTAC ERα Degrader-4 is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER + breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.
|
-
- HY-157569
-
|
PD-1/PD-L1
|
Cancer
|
PD1-PDL1-IN 2 (ZE132) is a potent and selective PD-1/PD-L1 inhibitor, which has robust anti-tumour activity in vivo. PD1-PDL1-IN 2 promotes cytotoxic T-cell tumour infiltration and induces IL-2 expression. In addition, PD1-PDL1-IN 2 elicits strong inhibitory effects on the mRNA expression of TGF-β .
|
-
- HY-15306AR
-
|
Thrombopoietin Receptor
Bacterial
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
Eltrombopag (Olamine) (Standard) is the analytical standard of Eltrombopag (Olamine). This product is intended for research and analytical applications. Eltrombopag Olamine (Eltrombopag diethanolamine salt) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag Olamine owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag Olamine can be used for the research of cardiovascular. Eltrombopag Olamine also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag Olamine can induce apoptosis in hepatocellular carcinomab (HCC) as well .
|
-
- HY-146295
-
|
COX
|
Inflammation/Immunology
|
COX-2/5-LOX-IN-2 (5b) is a potent and dual inhibitor of COX-2/5-LOX. COX-2/5-LOX-IN-2 is a benzothiophen-2-yl pyrazole carboxylic acid derivative. COX-2/5-LOX-IN-2 shows the most potent analgesic and anti-inflammatory activities surpassing that of Celecoxib and Indomethacin. COX-2/5-LOX-IN-2 shows potent COX-1, COX-2 and 5-LOX inhibitory activity with IC50s of 5.40, 0.01 and 1.78 μM, respectively .
|
-
- HY-146294
-
|
COX
|
Inflammation/Immunology
|
COX-2/5-LOX-IN-1 (compound 3a) is a potent and dual inhibitor of COX-2/5-LOX. COX-2/5-LOX-IN-1 is a benzothiophen-2-yl pyrazole carboxylic acid derivative. COX-2/5-LOX-IN-1 shows the most potent analgesic and anti-inflammatory activities surpassing that of Celecoxib and Indomethacin. COX-2/5-LOX-IN-1 shows potent COX-1, COX-2 and 5-LOX inhibitory activity with IC50s of 12.13, 0.4 and 4.96 μM, respectively .
|
-
- HY-152161
-
|
HIV
Reverse Transcriptase
|
Infection
|
HIV-1 inhibitor-51, a non-nucleoside reverse transcriptase inhibitor (NNRTI), exhibits outstanding antiviral activity against WT HIV-1 (IIIB) and a panel of mutant strains. HIV-1 inhibitor-51 has high binding affinity (KD=2.50 μM) and inhibitory activity (IC50=0.03 μM) to WT HIV-1 RT. HIV-1 inhibitor-51 has EC50s of 2.22-53.3 nM for mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, RES056) .
|
-
- HY-112823B
-
HS-10296 hydrochloride
|
EGFR
|
Cancer
|
Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer .
|
-
- HY-112823
-
HS-10296
|
EGFR
|
Cancer
|
Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
|
-
- HY-131909
-
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
CJ-2360 is a potent and orally active ALK inhibitor with IC50s of 2.2, 4.0, 8.8, 6.3, and 8.9 nM against wild-type ALK and F1197M, G1269A, L1196M, and S1206Y ALK mutants, respectively. CJ-2360 displays potent inhibitory activity against two clinically reported ALK mutants (C1156Y and L1196M) and a few other kinases (LTK, MERTK, CLK1, DAPK1, and DAPK2) among the 468 kinases evaluated .
|
-
- HY-N9521
-
|
Others
|
Cancer
|
3-O-β-D-Glucopyranosyl(1→2)-[a-Lrhamnopyranosyl(1→3)]-β-D-glucopyranosyl 28-O-β-D-glucuronopyranoside, a saponin, is isolated from Polaskia chichipe Backbg. 3-O-β-D-Glucopyranosyl(1→2)-[a-Lrhamnopyranosyl(1→3)]-β-D-glucopyranosyl 28-O-β-D-glucuronopyranoside shows ability to inhibit melanin biosynthesis by B16 melanoma cell with inhibitory activity 84.2% at 100μM[1].
|
-
- HY-138098
-
|
Others
|
Cancer
|
Sartorypyrone B is a 2β-acetoxyl analogue of chevalone C. Sartorypyrone B is yielded from the ethyl acetate extract of the culture of the marine sponge-associated fungus Neosartorya tsunodae (KUFC 9213). Sartorypyrone B exhibits strong growth inhibitory activity, having GI50s of 17.8, 20.5, and 25.0 μM, respectively, for MCF-7, NCI-H460, and A375-C5. Sartorypyrone B has the potential for the research of breast adenocarcinoma, non-small cell lung cancer, and melanoma diseases .
|
-
- HY-146001
-
|
Influenza Virus
|
Inflammation/Immunology
|
Influenza virus-IN-4 (compound 11e) is a potent influenza virus neuraminidase inhibitor with IC50s of 3.4, 0.094, 0.79, 0.077 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-4 shows NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-4 shows low cytotoxicity with an CC50 of >200 µM. Influenza virus-IN-4 shows no obvious toxicity at the dose of 1500 mg/kg in mice .
|
-
- HY-112823A
-
HS-10296 mesylate
|
EGFR
|
Cancer
|
Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer .
|
-
- HY-151262
-
|
JAK
STING
NF-κB
STAT
|
Inflammation/Immunology
|
JAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC50 values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitory activities against interferon-stimulated genes (ISG) and NF-κB pathways with IC50 values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD) .
|
-
- HY-151436
-
|
CDK
Cholinesterase (ChE)
Apoptosis
|
Cancer
|
ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC50 values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC50=19.023 μM) and BChE (IC50=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase .
|
-
- HY-151535
-
|
SARS-CoV
|
Infection
Inflammation/Immunology
|
SARS-CoV-2 3CLpro-IN-5 is a covalent inhibitor of 3C-like protease (3CL pro). SARS-CoV-2 3CLpro-IN-5 has inhibitory activity for 3CL pro with an IC50 value of 3.8 nM. SARS-CoV-2 3CLpro-IN-5 has 9.0% oral bioavailability (BA). SARS-CoV-2 3CLpro-IN-5 can be used for the research of coronavirus disease 2019 (COVID-19) .
|
-
- HY-149543
-
|
Mitochondrial Metabolism
Eukaryotic Initiation Factor (eIF)
Apoptosis
|
Cancer
|
BTM-3528 is an activator of the mitochondrial protease OMA1 and mediates excessive activation of the mitochondrial integrated stress response (ISR). BTM-3528 stimulates OMA1-dependent DELE1 and OPA1 cleavage and mitochondrial fragmentation. BTM-3528 activates eIF2α kinase HRI, inducing cell growth arrest and apoptosis. BTM-3528 has anticancer activity against multiple DLBCL cell lines and has in vivo inhibitory potency in a mouse model xenografted with human DLBCL SU-DHL-10 cells .
|
-
- HY-N1934
-
|
Potassium Channel
HSP
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .
|
-
- HY-146274
-
|
c-Met/HGFR
Apoptosis
|
Cancer
|
c-Met-IN-10 (compound 26a) is a highly potent c-Met kinase inhibitor with an IC50 value of 16 nM. c-Met-IN-10 has inhibitory activity against cancer cells A549, H460 and HT-29 with IC50s of 0.56 ~ 1.59 μM. c-Met-IN-10 suppresses the colony formation on HT-29 cells, induces HT-29 and A549 cells apoptosis, and inhibits A549 cells motility. c-Met-IN-10 can be used for researching anticancer .
|
-
- HY-P3492
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-34 (S-20-1) is a blood brain barrier penetrable pan-coronavirus (CoV) fusion inhibitor with broad-spectrum inhibitory activity. SARS-CoV-2-IN-34 effectively inhibits infection by pseudotyped and authentic SARS-CoV-2, and pseudotyped variants of concern (VOCs). SARS-CoV-2-IN-34 shows high affinity to RBD in S1 and HR1 domain in S2 of SARS-CoV-2 S protein. SARS-CoV-2-IN-34 can be used for the research of infection .
|
-
- HY-N10156
-
-
- HY-153460
-
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
TLR7/8/9 antagonist 2 is an orally active TLR7/8/9 antagonist. TLR7/8/9 antagonist 2 has inhibitory activities for HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC50 values of 0.011 μM, 0.029 μM and 0,052 μM, respectively.TLR7/8/9 antagonist 2 has high bioavailability in vivo.TLR7/8/9 antagonist 2 can be used for the research of auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis .
|
-
- HY-156457
-
|
EGFR
|
Cancer
|
EGFR-IN-90 (compound 34) is an orally active EGFR inhibitor. EGFR-IN-90 shows inhibitory activity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and inhibits the proliferation of the H1975-TM cell line harboring EGFRL858R/T790M/C797S with an IC50 of 0.05 μM. EGFR-IN-90 and inhibits tumor growth in the H1975-TM xenograft tumor model .
|
-
- HY-153857
-
|
FLT3
|
Cancer
|
PHI-101 is an orally active FLT3 inhibitor that overcomes resistance to multiple drug-resistant mutations. PHI-101 potently inhibits FLT3 single activating mutations (ITD or TKD mutants) and has inhibitory activity against FLT3 double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. PHI-101 has potential for research in relapsed or refractory acute myeloid leukemia (AML) .
|
-
- HY-162103
-
|
TAM Receptor
Apoptosis
|
Cancer
|
Axl-IN-18 (compound 25c) is a potent and selective type II AXL inhibitor. Axl-IN-18 shows excellent AXL inhibitory activity (IC50=1.1 nM) and 343-fold selectivity over the highly homologous kinase MET in biochemical assays (IC50=377 nM). Axl-IN-18 significantly inhibits AXL-driven cell proliferation, dose-dependently suppresses 4T1 cell migration and invasion, and induces apoptosis. Axl-IN-18 shows noticeable antitumor efficacy in a BaF3/TEL-AXL xenograft model .
|
-
- HY-N12820
-
|
Others
|
Cancer
|
3-O-6-Deoxy-3-O-methyl-β-D-allopyranosyl-(1→4)-β-D-oleandropyranosyl-tenacigenin C can be isolated from Alocasia cucullata (Lour.) G. Don. 3-O-6-Deoxy-3-O-methyl-β-D-allopyranosyl-(1→4)-β-D-oleandropyranosyl-tenacigenin C has moderate tumor cells inhibitory activity against MGC-803 and HT-29 cells with IC50 values of 45.6 and 28.4 μg/mL, respectively .
|
-
- HY-W052508
-
N-Desalkylquetiapine
|
5-HT Receptor
|
Neurological Disease
|
Norquetiapine is an antidepressant and neuroprotective agent and is the active metabolic component of Quetiapine (HY-14544). Norquetiapine is also a partial 5-HT1A receptor agonist, and a presynaptic α2, 5-HT2C and 5-HT7 b> Receptor antagonist. Norquetiapine can also selectively inhibit norepinephrine transporter (NET), inhibit norepinephrine reuptake, and has potential inhibitory effects on bipolar depression, major depressive disorder, and generalized anxiety disorder. Norquetiapine demonstrated in vivo activity in forced swimming in mice and learned helplessness tests in rats .
|
-
- HY-N8090
-
|
Others
|
Inflammation/Immunology
|
(3β,7β,12β,20Z)-3,7,12-Trihydroxy-11,15,23-trioxo-lanost-8,20-dien-26-oic acid, a lanostane triterpenoids, exhibits obvious NO inhibitory activity on n LPS-induced BV-2 microglia cells with an IC50 of 9.55 uM. (3β,7β,12β,20Z)-3,7,12-Trihydroxy-11,15,23-trioxo-lanost-8,20-dien-26-oic acid has anti-inflammatory activities .
|
-
- HY-144668
-
|
Influenza Virus
|
Infection
|
RdRP-IN-4 (compound 11q), an aryl benzoyl hydrazide analog, is an orally active influenza A virus RNA-dependent RNA polymerase (RdRp) inhibitor by interacting with the PB1 subunit. RdRP-IN-4 exhibits potent inhibitory activity against the avian H5N1 flu strain with an EC50 of 18 nM in MDCK cells. RdRP-IN-4 displays excellent potency against the the H1N1 (A/PR/8/34) Flu A strain and Flu B strain (B/Lee/1940) with EC50 values of 53 nM and 20 nM, respectively. RdRP-IN-4 significantly inhibits the expression level of viral nucleoprotein (NP) in a dose-dependent manner. RdRP-IN-4 exhibits significant antiviral activity in infected mice .
|
-
- HY-N2071
-
Cedrol
1 Publications Verification
(+)-Cedrol; α-Cedrol
|
Cytochrome P450
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes . Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities .
|
-
- HY-P1320
-
|
Opioid Receptor
|
Inflammation/Immunology
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
|
-
- HY-P1320A
-
|
Opioid Receptor
|
Inflammation/Immunology
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
|
-
- HY-144451
-
|
Trk Receptor
|
Cancer
|
TRK-IN-12 (Compound 9e) is a potent inhibitor of TRK (TRK G595R IC50 = 13.1 nM). TRK-IN-12 is a macrocyclic derivative compound. TRK-IN-12 shows significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC50 = 0.080 μM). TRK-IN-12 has shown a better inhibitory effect (IC50 = 0.646 μM) than control agent LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line .
|
-
- HY-143233
-
|
Pim
HDAC
Apoptosis
|
Cancer
|
PIM-1/HDAC-IN-1 (compound 4d) is a PIM-1 inhibitor, with an IC50 of 343.87 nM. PIM-1/HDAC-IN-1 has strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC50 values of 63.65 and 62.39 nM, respectively. PIM-1/HDAC-IN-1 exhibits apoptosis inducing potential in MCF-7 cell lines. PIM-1/HDAC-IN-1 shows pre-G1 apoptosis and cell cycle arrest at G2/M phase .
|
-
- HY-P1956
-
HSA
|
NF-κB
NO Synthase
|
Cardiovascular Disease
Inflammation/Immunology
|
Human serum albumin (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, NF-κB, and peroxynitrite (ONOO −) in the vascular wall, contributing to the reduction of blood pressure .
|
-
- HY-155846
-
|
Parasite
Bacterial
|
Infection
|
Antileishmanial agent-22 (compound 15b) is a parasite inhibitor and an antibacterial agent, with antileishmanial, antimalarial, and anti-tubercular activities. Antileishmanial agent-22 inhibits leishmanial (IC50=0.408 μM) based on antifolate mechanism. And, Antileishmanial agent-22 inhibits Folic acid and Folinic acid at 100 μM with inhibitory rates of 88% and 94%, respectively. Antileishmanial agent-22 inhibits P. berghei in vivo and in vitro, with 96.67% suppression under 48.4 μM/kg/day and 0.038 μM (IC50), respectively. Moreover, Antileishmanial agent-22 inhibits M. tuberculosis with MIC of 28.44 μM .
|
-
- HY-112823R
-
|
EGFR
|
Cancer
|
Almonertinib (Standard) is the analytical standard of Almonertinib. This product is intended for research and analytical applications. Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
|
-
- HY-145432
-
|
PI3K
|
Cancer
|
PI3K-IN-28 (Compound 6c) is a potent inhibitor of PI3K. PI3K-IN-28 displays the most potent activity with lower toxic effects on MCF-10a. PI3K-IN-28 displays half-maximal inhibitory concentration (IC50, μM) values of 5.8, 2.3, and 7.9. PI3K-IN-28 is the most potent one with a selectivity index (SI) of 39 and is considered as a latent lead for further optimization of anticancer agents .
|
-
- HY-146201
-
|
Phosphodiesterase (PDE)
|
Others
|
1 a /5-hydroxynitrile rubber 7 receptor antagonist (5-HT1 a k i = 8 nm, kb= 0.04 nm; 5-nitrile rubber 7K I = 451 nm, kb= 460 nm) has pde4b/pde7a inhibitory activity (PDE4B ic50= 80.4 μ M; Pde7a chip 50= 151.3 μ M)。 Compound 22 has a very good ability of passive penetration of biofilm and high metabolic stability in vitro. In addition, 22's pharmacological evaluation showed its pre cognitive and antidepressant properties in rat behavioral tests.
|
-
- HY-146019A
-
|
HIV
|
Infection
|
HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC50 of 13.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitory activity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC50 of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS .
|
-
- HY-101034
-
CHMFL-ABL-KIT-155
|
Bcr-Abl
c-Kit
Apoptosis
PDGFR
Discoidin Domain Receptor
|
Cancer
|
CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis .
|
-
- HY-149454
-
|
P2Y Receptor
|
Cancer
|
P2Y1/P2Y12 antagonist-1 (compound 24w) is an orally available dual inhibitor of P2Y1 and P2Y12 with antiplatelet activity. P2Y1/P2Y12 antagonist-1 inhibits ADP-induced platelet aggregation in rabbit plasma with an IC50 of 4.23 μM. P2Y1/P2Y12 antagonist-1 exhibits potent inhibitory effects in rat thrombosis model.
|
-
- HY-147913
-
|
PI3K
Akt
mTOR
Apoptosis
|
Cancer
|
PI3K/Akt/mTOR-IN-3 (compound 3d) is a potent PI3K/AKT/mTOR inhibitor. PI3K/Akt/mTOR-IN-3 displays the inhibitory activity in MCF-7, HeLa and HepG2 cells, with IC50 values of 0.77, 1.23, and 4.57μM, respectively. PI3K/Akt/mTOR-IN-3 inhibits the migration of MCF-7 and HeLa cells at the concentration of 4 μM. PI3K/Akt/mTOR-IN-3 induces cell apoptosis and S phase arrest .
|
-
- HY-151260
-
|
Beta-secretase
Cholinesterase (ChE)
GSK-3
|
Neurological Disease
|
AChE/BACE1/GSK3β-IN-1 is an orally active triple inhibitor of AChE/BACE1/GSK3β. AChE/BACE1/GSK3β-IN-1 has effective inhibitory activity against AChE, BACE1 and GSK3β with IC50 values of 1.0 μM, 20 μM and 15 μM, respectively. AChE/BACE1/GSK3β-IN-1 has good blood-brain barrier penetrability, suitable bioavailability. AChE/BACE1/GSK3β-IN-1 can be used for the research of Alzheimer's disease (AD) .
|
-
- HY-N4155
-
|
EBV
HIV Protease
HSV
|
Infection
Cancer
|
2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid, a natural ursane-type triterpene, is a potent inhibitor of HIV protease (HIV Protease). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid is also an inhibitor of the activation of Epstein-Barr virus early antigen (EBV-EA). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid displays an inhibitory activity against nitric oxide production in Lipopolysaccharide (Lipopolysaccharides)-activated RAW 264.7 cells .
|
-
- HY-135748A
-
|
Toll-like Receptor (TLR)
Apoptosis
|
Infection
Cancer
|
Poly (I:C):Kanamycin (1:1) sodium is an isometric complex of Poly (I:C) (HY-135748) and Kanamycin (HY-16566). Poly(I:C) sodium, a synthetic analog of double-stranded RNA, is a TLR3 and retinoic acid-inducible gene I receptor (RIG-I and b>MDA5) agonist. Poly(I:C) sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses and induce apoptosis in cancer cells . Kanamycin is an orally active antibacterial agent (Gram-negative/positive bacteria) that inhibits translocation and causes miscoding by binding to the 70S ribosomal subunit. Kanamycin shows good inhibitory activity against Mycobacterium tuberculosis (susceptible and drug-resistant) and Klebsiella pneumoniae, and can be used in the research of tuberculosis and pneumonia .
|
-
- HY-P5439
-
|
PKC
|
Others
|
Epsilon-V1-2, Cys-conjugated is a biological active peptide. (This peptide is the εPKC specific inhibitor. Its inhibitory activity is based on εPKC translocation and MARCKS phosphorylation. This peptide interferes with εPKC interaction with the anchoring protein εRACK. This peptide contains a cysteine residue added to the C-terminus for potential S-S bond formation with a carrier protein.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
|
-
- HY-155759
-
|
Others
|
Inflammation/Immunology
Cancer
|
HMGB1-IN-2 (compound 15) is an inhibitor of highly conserved nuclear protein (HMGB1), showing NO inhibitory effect with IC50 value of 20.2 μM in RAW264.7 cells. HMGB1-IN-2 (30 μM) decreases the level of IL-1 β, TNF-α, caspase-1 p20, inhibits the phosphorylation of NF-κB p65, exhibits anti-apoptotic activity. HMGB1-IN-2 (15 mg/kg; ip) relives kidney injury in septic acute kidney injury mouse. HMGB1-IN-2 inhibits Huh7 cells and A549 cells with IC50s of 77.0 μM, and 82.0 μM, respectively .
|
-
- HY-157432
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-97 (compound 6q) is a EGFR inhibitor. EGFR-IN-97 shows inhibitory activity against Ba/F3-EGFR L858R/T790M/C797S and Ba/F3-EGFR Del19/T790M/C797S cells, with IC50 values of 0.42 μM and 0.41 μM, respectively. EGFR-IN-97 can promote apoptosis of NCI-H1975-EGFR L858R/T790M/C797S cells at the concentration of 0.8 μM .
|
-
- HY-N2735
-
|
Influenza Virus
|
Infection
Inflammation/Immunology
|
7,3',4'-Trihydroxy-3-benzyl-2H-chromene is an reversible noncompetitive neuraminidase (NA) inhibitor. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene can be isolated from the dried heartwood of Caesalpinia sappan L. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene has potent NAs inhibitory activities with IC50 values of 34.6 µM [H1N1], 39.5 µM [H3N2], and 50.5µM [H9N2], respectively. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene can be used for the research of influenza virus .
|
-
-
-
HY-L051
-
|
947 compounds
|
Ferroptosis is a novel type of cell death program that is distinct from apoptosis, necroptosis and autophagy. It is dependent on iron and reactive oxygen species (ROS) and is characterized by lipid peroxidation. As a novel type of cell death, ferroptosis has distinct properties and recognizing functions involved in physical conditions or various diseases including cancers, neurodegenerative diseases, acute renal failure, etc.
MCE carefully collected a unique collection of 947 ferroptosis signaling pathway related compounds with ferroptosis-inducing or -inhibitory activity. MCE Ferroptosis Compound Library is a useful tool to study ferroptosis mechanism as well as related diseases.
|
Cat. No. |
Product Name |
Type |
-
- HY-P4202
-
Suc-AEPF-pNA
|
Chromogenic Substrates
|
Suc-Ala-Glu-Pro-Phe-pNA (Suc-AEPF-pNA) is a chromogenic substrate for the peptidylprolyl isomerase Pin1. Suc-Ala-Glu-Pro-Phe-pNA can be used to evaluate the inhibitory effect of the target compound on Pin1, and catalytic activity of Pin1, etc .
|
-
- HY-P4202A
-
Suc-AEPF-pNA TFA
|
Chromogenic Substrates
|
Suc-Ala-Glu-Pro-Phe-pNA (Suc-AEPF-pNA ) TFA is a chromogenic substrate for the peptidylprolyl isomerase Pin1. Suc-Ala-Glu-Pro-Phe-pNA TFA can be used to evaluate the inhibitory effect of the target compound on Pin1, and catalytic activity of Pin1, etc .
|
-
- HY-D2204
-
|
Fluorescent Dyes/Probes
|
SHP1-IN-1 (compound 5p) is a fluorescent probe for the protein tyrosine phosphatase SHP1 containing the Src homology 2 domain. SHP1-IN-1 has SHP1 inhibitory activity, selectivity for Fe 3+ ions and good fluorescence properties. SHP1-IN-1 exhibits aggregation post-quenching (ACQ) effect, good interference immunity and low detection limit (5.55 μM) .
|
Cat. No. |
Product Name |
Type |
-
- HY-P1956
-
HSA
|
Native Proteins
|
Human serum albumin (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, NF-κB, and peroxynitrite (ONOO −) in the vascular wall, contributing to the reduction of blood pressure .
|
-
- HY-W354851
-
|
Biochemical Assay Reagents
|
Pisiferic acid is an antibacterial agent with inhibitory activity against Gram-negative/positive bacteria such as P. vulgaris, S. aureus and B. subtilis. Pisiferic acid can be used to study bacterial infections .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2157
-
|
Ras
|
Cancer
|
Ras Inhibitory Peptide (VPPPVPPRRR) is a Ras inhibitor with antitumor activity .
|
-
- HY-P10242
-
|
Peptides
|
Others
|
Myostatin inhibitory peptide 7 is a recombinant protein comprised of activin receptor type IIB (ActRIIB) linked to the Fc region of human immunoglobulin IgG1. Myostatin inhibitory peptide 7 exhibits inhibitory activity against myostatin and other negative regulators of muscle mass, promotes muscle growth .
|
-
- HY-P3578
-
|
Insulin Receptor
|
Endocrinology
|
Gastric Inhibitory Polypeptide (1-30), porcine lacks the C-terminal 12 amino acid residues of natural gastric inhibitory polypeptide (GIP), exhibits biologic activity by potentiating the release of insulin and somatostatin .
|
-
- HY-114437
-
Z-D-Phe-Phe-Gly-OH; FIP; Virus Replication inhibitory Peptide
|
Influenza Virus
|
Infection
|
Fusion Inhibitory Peptide (Z-D-Phe-Phe-Gly-OH, FIP, Virus Replication Inhibitory Peptide) is a potent inhibitor of the virus replication, by inhibiting the membrane fusing activity of a viral glycoprotein .
|
-
- HY-143884
-
|
JAK
|
Inflammation/Immunology
|
JAK2/TYK2-IN-2 is a potent and selective TYK2 inhibitor with IC50 values of 9 and 157 nM for TYK2 and JAK2, respectively. JAK2/TYK2-IN-2 has anti-inflammatory activity .
|
-
- HY-P1547
-
|
Peptides
|
Neurological Disease
|
Somatostatin-25 is a endogenous neuropeptide hormone that shows inhibitory activity against secretion of growth hormone.
|
-
- HY-P4810
-
T140
|
CXCR
|
Infection
|
Polyphemusin II-Derived Peptide (T140), a CXCR4 inhibitor, shows high inhibitory activity against HIV-1 entry and the inhibitory effect on the binding of an anti-CXCR4 monoclonal antibody (12G5) to CXCR4 .
|
-
- HY-P4488
-
|
Peptides
|
Others
|
H-Pro-Pro-Gln-OH is a oligopeptide with excellent dipeptidyl peptidase-IV (DPP-IV) inhibitory activity .
|
-
- HY-P10159
-
|
Bacterial
|
Infection
|
Diplacol ia a natural compound from from Mimulus clevelandi and shows potent inhibitory activities against lipopolysaccharide (LPS)-induced nitric oxide production .
|
-
- HY-P5107
-
|
VEGFR
|
Cancer
|
Protein LMWP is a cell-penetrating peptide with vascular endothelial growth factor (VEGF) inhibitory activity. Protein LMWP can inhibit tumor growth and is used in cancer research .
|
-
- HY-P10447
-
Fengycin IX; SNA-60-367-3
|
Phospholipase
|
Inflammation/Immunology
|
Plipastatin A1 is a lipopeptide with enzyme inhibitory and immunosuppressive activities. Plipastatin A1 is found in Bacillus cereus and inhibits phospholipase A2 (PLA2), PLC, and PLD .
|
-
- HY-P3985
-
Bradykinin potentiating peptide B
|
Angiotensin-converting Enzyme (ACE)
|
Others
|
Bradykinin potentiator B (Bradykinin potentiating peptide B) is venom of Agkistrodon halys blomhoffi. Bradykinin potentiator B is a potent ACE inhibitor. Bradykinin potentiator inhibits the activity of bradykinin inhibitory peptidase .
|
-
- HY-P5286
-
|
Bacterial
|
Infection
Cancer
|
BMAP-27 is an antimicrobial peptide capable of disrupting the membrane integrity of microorganisms. Due to its membrane permeability, MAP-27 has inhibitory activity against both bacteria and cancer cells .
|
-
- HY-P10202
-
|
STAT
|
Cancer
|
5-FAM-GpYLPQTV-NH2 is a fluorescently labeled peptide and has STAT3 inhibitory activity. 5-FAM-GpYLPQTV-NH2 can be used in cancer research .
|
-
- HY-P4874
-
|
Melanocortin Receptor
|
Metabolic Disease
|
ACTH (7-38) (human) is the 7-38 fragment of human ACTH (1-39). human ACTH (1-39), known as a corticotropin inhibitory peptide (CIP), is an antagonist of the ACTH receptor and has no any corticosteroid activity .
|
-
- HY-P10202A
-
|
STAT
|
Cancer
|
5-FAM-GpYLPQTV-NH2 (TFA) is a fluorescently labeled peptide and has STAT3 inhibitory activity. 5-FAM-GpYLPQTV-NH2 (TFA) can be used in cancer research .
|
-
- HY-P10434
-
BRC4 repeat motif
|
Peptides
|
Cancer
|
BRC4wt (BRC4 repeat motif) is part of the BRACA2 tumor suppressor protein, which exhibits inhibitory activity against interaction of the BRACA2 protein with RAD51, and is involved in the repair of DNA damage .
|
-
- HY-P5016
-
|
Antibiotic
Bacterial
Fungal
|
Infection
Cancer
|
CRAMP-18 (mouse) is an antibiotic peptide without hemolytic activity. CRAMP-18 (mouse) has good inhibitory activity against Gram-negative bacteria, such as S. typhimurium and P. aeruginosa. CRAMP-18 (mouse) has the potential to study antifungal, antibacterial and antitumor .
|
-
- HY-P1149
-
Epithalon; Epithalamin
|
Telomerase
|
Neurological Disease
Cancer
|
Epitalon is an anti-aging agent and a telomerase activator. Epitalon has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon can be used for cancer, old age and Retinitis Pigmentosa .
|
-
- HY-P1149A
-
Epithalon TFA; Epithalamin TFA
|
Telomerase
|
Neurological Disease
Cancer
|
Epitalon TFA is an anti-aging agent and a telomerase activator. Epitalon TFA has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon TFA can be used for cancer, old age and Retinitis Pigmentosa .
|
-
- HY-P4095
-
|
CXCR
|
Cancer
|
NoxaBH3 is a cysteine-based cross-linked peptide with increased cell permeability and higher inhibitory activity against Mcl-1. NoxaBH3 binds to the endogenous CXCR4 ligand to produce ubiquitin-Noxabh3 conjugate. NoxaBH3 is then delivered to cancer cells .
|
-
- HY-P4202
-
Suc-AEPF-pNA
|
Biochemical Assay Reagents
|
Others
|
Suc-Ala-Glu-Pro-Phe-pNA (Suc-AEPF-pNA) is a chromogenic substrate for the peptidylprolyl isomerase Pin1. Suc-Ala-Glu-Pro-Phe-pNA can be used to evaluate the inhibitory effect of the target compound on Pin1, and catalytic activity of Pin1, etc .
|
-
- HY-103502
-
|
GABA Receptor
|
Neurological Disease
|
CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. CGP7930 enhances the inhibitory effect of l-baclofen on the oscillatory activity of cultured cortical neurons .
|
-
- HY-P4202A
-
Suc-AEPF-pNA TFA
|
Biochemical Assay Reagents
|
Others
|
Suc-Ala-Glu-Pro-Phe-pNA (Suc-AEPF-pNA ) TFA is a chromogenic substrate for the peptidylprolyl isomerase Pin1. Suc-Ala-Glu-Pro-Phe-pNA TFA can be used to evaluate the inhibitory effect of the target compound on Pin1, and catalytic activity of Pin1, etc .
|
-
- HY-P0111
-
Z-WE(OMe)HD(OMe)-FMK
|
Caspase
Cathepsin
|
Cancer
|
Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis .
|
-
- HY-103295
-
|
Bradykinin Receptor
|
Metabolic Disease
Inflammation/Immunology
|
Lys-[Des-Arg9]Bradykinin, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin has low inhibitory activity on B2 receptors .
|
-
- HY-P6177
-
|
Dipeptidyl Peptidase
|
Inflammation/Immunology
|
SGP8 (IAVPGEVA) is an octopeptide derived from the hydrolysis of soybean 11S globulin. SGP8 (IAVPGEVA) has the role of regulating lipid metabolism, inflammation and fibrosis. SGP8 (IAVPGEVA) exhibits inhibitory activity against DPP4 and inhibits the JNK-c-Jun signaling pathway. SGP8 (IAVPGEVA) has the ability to inhibit the non-alcoholic steatohepatitis (NASH) .
|
-
- HY-103295A
-
|
Bradykinin Receptor
|
Metabolic Disease
Inflammation/Immunology
|
Lys-[Des-Arg9]Bradykinin TFA, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin TFA has low inhibitory activity on B2 receptors .
|
-
- HY-P5483
-
|
Bacterial
|
Others
|
Retro-indolicidin is a biological active peptide. (Reverse peptide of indolicidin (Rev4) is a 13-amino acid residue peptide based on the sequence of indolicidin. Indolicidin, a member of the cathelicidin protein family, is a 13-amino acid residue cationic, antimicrobial peptide-amide isolated from the cytoplasmic granules of bovine neutrophils. The synthetic peptide Rev4 has been shown to possess strong antimicrobial as well as protease inhibitory activities in vitro.)
|
-
- HY-P4641
-
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
H-Trp-Phe-OH is a dipeptide consisting of tryptophan and phenylalanine (Trp-Phe). H-Trp-Phe-OH is also an antihypertensive peptide with inhibitory activity on angiotensin-converting enzyme (ACE), dose-dependently increases NO levels, and decreases endothelin-1 (ET-1) levels. H-Trp-Phe-OH (2 mg/kg; subcutaneous injection; 6 injections over 3 days) causes an increase in ovarian weight in female mice .
|
-
- HY-P2302
-
|
Antibiotic
Bacterial
Fungal
|
Infection
|
Defensin HNP-3 human is a cytotoxic antibiotic peptide known as "defensin". Defensin HNP-3 human has inhibitory activity against Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. Defensin HNP-3 human is initially synthesized as the 94 amino acids preproHNP(1-94), which is hydrolyzed to proHNP(20-94) and converted to mature HNP(65-94) after the removal of anion precursors .
|
-
- HY-12403
-
Talfirastide
Maximum Cited Publications
9 Publications Verification
TXA127; Angiotensin (1-7); Ang-(1-7)
|
Angiotensin Receptor
Angiotensin-converting Enzyme (ACE)
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
|
Angiotensin 1-7 (Ang-(1-7)) is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 inhibits purified canine ACE activity (IC50=0.65 μM). Angiotensin 1-7 acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium. Angiotensin 1-7 shows anti-inflammatory activity .
|
-
- HY-12403A
-
TXA127 acetate; Angiotensin (1-7) (acetate); Ang-(1-7) (acetate)
|
Angiotensin Receptor
Angiotensin-converting Enzyme (ACE)
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
|
Angiotensin 1-7 (Ang-(1-7)) acetate is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 acetate inhibits purified canine ACE activity (IC50=0.65 μM). Angiotensin 1-7 acetate acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 acetate blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium .
|
-
- HY-P10281
-
|
Bacterial
|
Infection
|
RW3 is a small cationic hexapeptide with amphiphilic properties. RW3 targets the plasma membrane of bacteria and works by inhibiting cell respiration and cell wall synthesis. RW3 shows high biological activity against gram-positive bacteria and does not show significant cytotoxic or hemolytic effects in previous studies. RW3 quickly kills 97% of the initial colony forming units (CFU) within 10 minutes at twice the minimum inhibitory concentration (MIC). RW3 can be used in antimicrobial and antifungal studies .
|
-
- HY-P3492
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-34 (S-20-1) is a blood brain barrier penetrable pan-coronavirus (CoV) fusion inhibitor with broad-spectrum inhibitory activity. SARS-CoV-2-IN-34 effectively inhibits infection by pseudotyped and authentic SARS-CoV-2, and pseudotyped variants of concern (VOCs). SARS-CoV-2-IN-34 shows high affinity to RBD in S1 and HR1 domain in S2 of SARS-CoV-2 S protein. SARS-CoV-2-IN-34 can be used for the research of infection .
|
-
- HY-P1320
-
|
Opioid Receptor
|
Inflammation/Immunology
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
|
-
- HY-P1320A
-
|
Opioid Receptor
|
Inflammation/Immunology
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
|
-
- HY-P5439
-
|
PKC
|
Others
|
Epsilon-V1-2, Cys-conjugated is a biological active peptide. (This peptide is the εPKC specific inhibitor. Its inhibitory activity is based on εPKC translocation and MARCKS phosphorylation. This peptide interferes with εPKC interaction with the anchoring protein εRACK. This peptide contains a cysteine residue added to the C-terminus for potential S-S bond formation with a carrier protein.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
- HY-N12472
-
-
- HY-N6890
-
-
- HY-N5063
-
-
- HY-N12134
-
-
- HY-105463
-
|
Quinones
Structural Classification
Microorganisms
Anthraquinones
Source classification
|
Antibiotic
Bacterial
|
Saptomycin D is an antibiotic with antitumor activity isolated from the Streptomyces sp. HP530 strain. Saptomycin D exhibits potent inhibitory effects against Gram-positive bacteria, while demonstrating weaker inhibitory activities against certain Gram-negative bacteria and yeasts. Saptomycin D also displays remarkable antitumor properties. Saptomycin D is applicable in research within the field of oncology .
|
-
- HY-130787
-
-
- HY-121020
-
-
- HY-N10192
-
-
- HY-N9314
-
-
- HY-N8024
-
-
- HY-N9528
-
-
- HY-126455
-
-
- HY-N1158
-
-
- HY-N12262
-
-
- HY-N5075
-
-
- HY-N2266
-
-
- HY-N10448
-
-
- HY-114336
-
-
- HY-Y0790
-
-
- HY-N9317
-
-
- HY-N8184
-
-
- HY-N12263
-
-
- HY-N11965
-
-
- HY-N12361
-
-
- HY-N12398
-
-
- HY-N8535
-
-
- HY-125732
-
-
- HY-N8018
-
-
- HY-N2039
-
-
- HY-N8209
-
-
- HY-N3643
-
-
- HY-N12511
-
-
- HY-N0616
-
-
- HY-114798
-
-
- HY-N2010
-
-
- HY-B0125
-
-
- HY-119821
-
-
- HY-N1547
-
-
- HY-N10453
-
-
- HY-N10454
-
-
- HY-N8619
-
-
- HY-119458
-
-
- HY-N8092
-
-
- HY-B0222
-
-
- HY-N0555
-
-
- HY-N7203
-
-
- HY-N2058
-
-
- HY-N4136
-
-
- HY-N6621
-
-
- HY-N4168A
-
-
- HY-126983
-
-
- HY-N12600
-
-
- HY-N12737
-
-
- HY-100385
-
-
- HY-W001542
-
-
- HY-N6310
-
-
- HY-N9535A
-
-
- HY-N7346
-
-
- HY-N0136
-
-
- HY-N7989
-
-
- HY-N10128
-
-
- HY-N10275
-
-
- HY-N3674
-
-
- HY-N3091
-
-
- HY-N9036
-
-
- HY-N12618
-
-
- HY-138100
-
-
- HY-B0502A
-
-
- HY-N10274
-
-
- HY-N10285
-
-
- HY-N11552
-
-
- HY-N11940
-
-
- HY-N11993
-
-
- HY-N12636
-
-
- HY-115770
-
-
- HY-N0136A
-
-
- HY-N9324
-
-
- HY-W047478
-
-
- HY-N8669
-
-
- HY-N8984
-
-
- HY-N3574
-
-
- HY-N0136B
-
-
- HY-N3518
-
-
- HY-N7628
-
-
- HY-N11637
-
-
- HY-N2809
-
-
- HY-N3211
-
-
- HY-N7324
-
-
- HY-N8007
-
-
- HY-N12637
-
-
- HY-113614
-
-
- HY-N2621
-
-
- HY-N7505
-
-
- HY-N1510
-
-
- HY-N6891
-
-
- HY-N0495
-
-
- HY-W009248
-
-
- HY-N5051
-
-
- HY-N1162
-
-
- HY-N10340
-
-
- HY-N11841
-
-
- HY-N2703
-
-
- HY-155410
-
-
- HY-113053
-
-
- HY-12136
-
-
- HY-N1098
-
-
- HY-N1120
-
-
- HY-N10292
-
-
- HY-N11994
-
-
- HY-N12527
-
-
- HY-N12723
-
-
- HY-N7272
-
-
- HY-N11771
-
-
- HY-N1549
-
-
- HY-N8104
-
-
- HY-126989
-
-
- HY-N8406
-
|
Microorganisms
Source classification
Phenols
|
Bacterial
Antibiotic
|
Monomethylsulochrin is a potent antibacterial metabolite from endophytic fungus Aspergillus fumigatus, isolated from Albizia lucidior leaves (fabaceae). Monomethylsulochrin exhibits anti-Staphylococcus aureus activity with minimum inhibitory concentration (MIC) of 31.25 μg/mL .
|
-
- HY-N8646
-
-
- HY-N10097
-
-
- HY-N11892
-
-
- HY-W745164
-
-
- HY-N1170
-
-
- HY-N2658
-
-
- HY-N10108
-
-
- HY-N8523
-
-
- HY-N6252
-
-
- HY-N2481
-
-
- HY-118463
-
-
- HY-N10472
-
-
- HY-N8329
-
-
- HY-N2443
-
-
- HY-N11128
-
-
- HY-125300
-
-
- HY-N3014
-
-
- HY-N2298
-
-
- HY-N7430
-
-
- HY-N9404
-
-
- HY-N10755A
-
-
- HY-N0223
-
-
- HY-113632
-
-
- HY-N2906
-
-
- HY-N12200
-
-
- HY-N12347
-
-
- HY-126462
-
-
- HY-N3185
-
-
- HY-N12507
-
-
- HY-N1186
-
-
- HY-N0501
-
-
- HY-N2472
-
-
- HY-N8167
-
-
- HY-N12070
-
-
- HY-N7072
-
-
- HY-137823
-
-
- HY-N8850
-
-
- HY-N2902
-
|
Structural Classification
Flavonols
Flavonoids
Source classification
Plants
Moraceae
|
Others
|
Artocarpin is an isoprenoid-substituted flavonoid, that can be isolated from the wood of Artocarpus heterophyllus. Artocarpin inhibits melanin biosynthesis in B16 melanoma cells without inhibiting tyrosinase. The presence of the isoprenoid-substituted moiety enhanced the inhibitory activity on melanin production in B16 melanoma cells .
|
-
- HY-155704
-
-
- HY-N6797
-
-
- HY-146036
-
-
- HY-N9051
-
-
- HY-N1839
-
-
- HY-N6972
-
-
- HY-N0577
-
-
- HY-N1416
-
-
- HY-111934
-
-
- HY-N11441
-
-
- HY-N4061
-
-
- HY-N0854
-
-
- HY-N1517
-
-
- HY-N0646
-
-
- HY-126564
-
-
- HY-N12915
-
-
- HY-118747
-
-
- HY-N11999
-
-
- HY-N0817
-
-
- HY-B0778
-
-
- HY-106888
-
-
- HY-N3841
-
-
- HY-B0856
-
-
- HY-N10335
-
-
- HY-126535
-
-
- HY-N12390
-
-
- HY-112661
-
-
- HY-N0041
-
-
- HY-N0828
-
-
- HY-N3348
-
-
- HY-134008
-
-
- HY-N12320
-
-
- HY-16566A
-
-
- HY-N7110
-
-
- HY-N6257
-
-
- HY-N3243
-
-
- HY-N3244
-
-
- HY-N1636
-
-
- HY-N7844
-
-
- HY-N7160
-
-
- HY-N3841A
-
-
- HY-N7150
-
5,7-Dihydroxy-3',4',5'-trimethoxyflavone
|
Structural Classification
Flavonols
Haplopteris anguste-elongata (Hayata) E. H. Crane
Flavonoids
Chrysanthemum × morifolium (Ramat.) Hemsl.
Source classification
Pteridaceae
Plants
Compositae
|
Xanthine Oxidase
|
Tricetin 3',4',5'-trimethyl ether (5,7-Dihydroxy-3',4',5'-trimethoxyflavone) is a flavone glucoside, that can be isolated the flowers of Chrysanthemum sinensea. Tricetin 3',4',5'-trimethyl ether displays xanthine oxidase competitive-type inhibitory activity, with an IC50 of 0.51 μM and a Ki of 0.37 μM .
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- HY-N12726
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- HY-N2284
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Flavonols
Flavonoids
Classification of Application Fields
Leguminosae
Source classification
Phenols
Polyphenols
Plants
Sophora flavescens Aiton
Disease Research Fields
Cancer
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Cholinesterase (ChE)
Beta-secretase
Phosphodiesterase (PDE)
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Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC50 of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 µM, 0.17 µM, 17.89 µg/mL, 10.98 µM, 8.37 µM and 8.21 µM, respectively.
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- HY-N1735
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- HY-N0632
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- HY-N6924
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- HY-N4215
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- HY-N0970
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Source classification
Erigeron canadensis L.
Plants
Compositae
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Others
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(4Z)-Lachnophyllum lactone is a enyne derivative. (4Z)-Lachnophyllum lactone shows growth inhibitory activity against Lemna paucicostata (IC50=104 μM), which is a problematic and invasive weed . (4Z)-Lachnophyllum lactone is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-N12161
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- HY-N12198
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Structural Classification
Natural Products
Microorganisms
Source classification
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Others
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Mollicellin H is a secondary metabolite of the fungus C. brasiliense and has a wide range of biological activities, including immunomodulation, cytotoxicity and anti-tumor effects. The growth inhibitory effects (GI50s) of Mollicellin H on human breast cancer (Bre04), human lung (Lu04) and human neuroma (N04) cell lines are 5.1 μg/mL, 6.5 μg/mL and 2.5 μg/mL respectively .
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- HY-N0057
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3,4-Di-O-caffeoylquinic acid; Isochlorogenic acid B
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Infection
Caprifoliaceae
Classification of Application Fields
Ketones, Aldehydes, Acids
Source classification
Phenols
Polyphenols
Plants
Endogenous metabolite
Disease Research Fields
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Glucosidase
Influenza Virus
Apoptosis
Endogenous Metabolite
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3,4-Dicaffeoylquinic acid (3,4-Di-O-caffeoylquinic acid), naturally isolated from Laggera alata, has antioxidative, DNA protective, neuroprotective and hepatoprotective properties. 3,4-Dicaffeoylquinic acid exerts apoptosis-mediated cytotoxicity and α-glucosidase inhibitory effects. 3,4-Dicaffeoylquinic acid possesses a unique mechanism of anti-influenza viral activity, that is, enhancing viral clearance by increasing TRAIL .
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- HY-N0619
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- HY-N0241
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- HY-N1773
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- HY-N11957
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- HY-N10439
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- HY-N10503
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Structural Classification
Flavonoids
Flavones
Plants
Moraceae
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Tyrosinase
Ras
Raf
MAPKAPK2 (MK2)
Apoptosis
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Norartocarpetin is a tyrosinase inhibitor. Norartocarpetin has strong tyrosinase inhibitory activity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells .
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- HY-152120
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Aiphanol
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Structural Classification
Source classification
Phenols
Polyphenols
Arecaceae
Plants
Aiphanes aculeata Willd
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COX
VEGFR
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(±)-Aiphanol is a newly discovered stilbenolignan analog. (±)-Aiphanol exhibits significant anti-inflammatory activity, acting through inhibition of COX-1 and COX-2. The inhibitory effect on COX-1 (IC50 = 1.9 μM) is particularly strong, while the effect on COX-2 (IC50= 9.9 μM) is relatively weak .(±)-Aiphanol effectively inhibits VEGFR2 (IC50=0.92 µM). (±)-Aiphanol blocks angiogenesis and promotes apoptosis through inhibition of VEGFR2 and COX2 activity. (±)-Aiphanol is orally active .
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- HY-N0005
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- HY-N2025
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- HY-N1365
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- HY-N0396
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- HY-N1783
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Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
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Phosphatase
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(24E)-3,4-Secocucurbita-4,24-diene-3,26,29-trioic acid is a potent PTP1B inhibitor, with an IC50 of 0.4 μM. (24E)-3,4-Secocucurbita-4,24-diene-3,26,29-trioic acid exhibits potent PTP1B inhibitory activity without cytotoxicity .
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- HY-N0041R
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- HY-N12606
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- HY-12403
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- HY-100513A
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- HY-12403A
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- HY-N0619A
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- HY-N0930B
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- HY-N10868
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- HY-N3364
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- HY-N0568
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- HY-B1890
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- HY-N12964
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Structural Classification
Alkaloids
Simaroubaceae
Ailanthus altissima (Mill.) Swingle
Source classification
Quinoline Alkaloids
Plants
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Others
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4-Hydroxycanthin-6-one is a novel quinoline alkaloid isolated from the stem bark of the tree Ailanthus altissima. Five other known compounds were also found in the study. The structures of the new compounds were determined by interpretation of physical and spectroscopic data, and their absolute configurations were determined by electronic circular dichroism spectroscopy and quantum chemical calculations. These compounds showed significant inhibitory activity against lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells, showing potential anti-inflammatory properties .
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- HY-N0058
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- HY-N9521
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- HY-138098
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- HY-N1934
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- HY-N10156
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- HY-N12820
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- HY-N8090
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Triterpenes
Microorganisms
Classification of Application Fields
Terpenoids
Source classification
Disease Research Fields
Inflammation/Immunology
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Others
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(3β,7β,12β,20Z)-3,7,12-Trihydroxy-11,15,23-trioxo-lanost-8,20-dien-26-oic acid, a lanostane triterpenoids, exhibits obvious NO inhibitory activity on n LPS-induced BV-2 microglia cells with an IC50 of 9.55 uM. (3β,7β,12β,20Z)-3,7,12-Trihydroxy-11,15,23-trioxo-lanost-8,20-dien-26-oic acid has anti-inflammatory activities .
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- HY-N2071
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Cedrol
1 Publications Verification
(+)-Cedrol; α-Cedrol
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Cedrus deodara (Roxburgh) G. Don
Classification of Application Fields
Pinaceae
Terpenoids
Sesquiterpenes
Source classification
Plants
Inflammation/Immunology
Disease Research Fields
Cancer
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Cytochrome P450
Fungal
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Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes . Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities .
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- HY-N4155
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Rosaceae
Rosa cymosa (L.) Tratt.
Plants
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EBV
HIV Protease
HSV
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2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid, a natural ursane-type triterpene, is a potent inhibitor of HIV protease (HIV Protease). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid is also an inhibitor of the activation of Epstein-Barr virus early antigen (EBV-EA). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid displays an inhibitory activity against nitric oxide production in Lipopolysaccharide (Lipopolysaccharides)-activated RAW 264.7 cells .
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- HY-N2735
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Structural Classification
Leguminosae
Caesalpinia sappan L.
Source classification
Phenols
Polyphenols
Plants
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Influenza Virus
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7,3',4'-Trihydroxy-3-benzyl-2H-chromene is an reversible noncompetitive neuraminidase (NA) inhibitor. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene can be isolated from the dried heartwood of Caesalpinia sappan L. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene has potent NAs inhibitory activities with IC50 values of 34.6 µM [H1N1], 39.5 µM [H3N2], and 50.5µM [H9N2], respectively. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene can be used for the research of influenza virus .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-101404S
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DL-Homocysteine thiolactone-d4 hydrochloride is the deuterium labeled DL-Homocysteine thiolactone (hydrochloride). DL-Homocysteine thiolactone hydrochloride is a cyclic amino acid derivative that exhibits root-growth inhibitory activity.
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- HY-14874S
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Topiroxostat-d4 is deuterium labeled Topiroxostat. Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment[1][2].
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- HY-N0893S
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Tetrahydrocurcumin-d6 is a deuterium labeled Tetrahydrocurcumin. Tetrahydrocurcumin is a Curcuminoid which displays inhibitory activity for CYP2C9 and CYP3A4[1].
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- HY-N0136S
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Taxifolin-d3 is deuterium labeled Taxifolin. Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM[1]. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity[2].
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- HY-Y0790S
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Cuminaldehyde-d8 is deuterated labeled Cuminaldehyde (HY-Y0790). Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity .
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- HY-100659S
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Dihydrodiol-Ibrutinib-d5 is the deuterium labeled Dihydrodiol-Ibrutinib (HY-100659). Dihydrodiol-Ibrutinib is a dihydrodiol active metabolite of Ibrutinib (HY-10997), has inhibitory activity towards BTK approximately 15 times lower than that of ibrutinib .
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- HY-W015307S
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4-Ethyloctanoic acid- 13C2 is 13C labeled Cuminaldehyde (HY-Y0790). Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity .
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- HY-B0673S
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Pirfenidone-d5 is a deuterium labeled Pirfenidone. Pirfenidone is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities[1][2][3].
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- HY-N0136S1
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(±)-Taxifolin-13C3 ((±)-Dihydroquercetin-13C3) is a derivative of (±)-Taxifolin, labeled with 13C3. (±)-Taxifolin is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
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- HY-N0005S
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Curcumin-d6is a deuterium labeled Curcumin (Turmeric yellow). Curcumin (Turmeric yellow) is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase (HATs) and also shows inhibitory effects on NF-κB and MAPKs.
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- HY-14956S
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Nemonoxacin-d3 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia[1][2][3].
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- HY-14956S2
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Nemonoxacin-d4 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia[1][2][3].
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- HY-10235S
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Telaprevir-d4 is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide[1][2][3]. Telaprevir inhibits SARS-CoV-2 3CLpro activity[4].
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- HY-14956S1
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Nemonoxacin-d3-1 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia[1][2][3].
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- HY-15306S
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1 Publications Verification
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Eltrombopag- 13C4 (SB-497115- 13C4) is 13 sup>C-labeled Z-Eltrombopag. Z-Eltrombopag is an orally active thrombopoietin-receptor non-peptide agonist with platelet-stimulating activity for the study of chronic immune thrombocytopenia. Eltrombopag also has strong inhibitory effects on multidrug-resistant Staphylococcus aureus (Staphylococcus aureus) and can induce apoptosis (apoptosis) in liver cancer cells .
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- HY-B1138S
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Fenbufen-d9 (CL-82204-d9) is the deuterium labeled Fenbufen. Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor[1][2][3][4][5].
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Cat. No. |
Product Name |
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Classification |
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- HY-162356
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Azide
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PD-L1-IN-4 (Compound X18) is an orally active PD-L1 inhibitor that exhibits remarkable inhibitory activity against the PD-1/PD-L1 interaction (IC50 = 1.3 nM) and enhances PD-L1 inhibitory effect on T cells (EC50 = 152.8 nM). PD-L1-IN-4 can be used for the research of cancer .
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- HY-149057
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Azide
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NDV-IN-1 is an antiviral agent with high neuraminidase inhibitory activity. NDV-IN-1 exhibits in vitro inhibitory activity against Newcastle disease virus (NDV). NDV-IN-1 significantly inhibits NDV infection of Vero cells by preventing the release of virus particles from infected cells . Neuraminidase-IN-12 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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