Search Result
Results for "
ICR
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-19336
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Epigenetic Reader Domain
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Cancer
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BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe .
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- HY-151563A
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Deubiquitinase
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Cancer
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OTUB1/USP8-IN-1 TFA is the TFA salt form of OTUB1/USP8-IN-1 (HY-151563). OTUB1/USP8-IN-1 TFA is a dual inhibitor for OTUB1/USP8, IC50 for OTUB1 and USP8 is 0.17 and 0.28 nM, respectively. OTUB1/USP8-IN-1 TFA inhibits proliferation of NSCLC cells. OTUB1/USP8-IN-1 TFA exhibits good pharmacokinetic characters in ICR mouse, and exhibits antitumor activity in H1975 xenograft mouse model .
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- HY-161539
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Opioid Receptor
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Neurological Disease
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KOR agonist 1 (Compound 7a) is a selective agonist for opioid receptor, with EC50s of 3.4, 701.2 and 1649 nM, for KOR, MOR and DOR, respectively. KOR agonist 1 binds KOR, MOR and DOR, with Kis of 3.9, 1053 and 4196 nM, respectively. KOR agonist 1 exhibits antinociceptive effect in ICR mouse model (ED50 in hot plate test is 0.3 mg/kg, in abdominal constriction test is 0.2 mg/kg) .
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- HY-163315
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Keap1-Nrf2
AMPK
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Metabolic Disease
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YPLP is a yeast-derived peptide Tyr-Pro-Leu-Pro, which exhibits activity in anti fatigue mechanisms through the nuclear factor erythroid-2-related factor 2 (Nrf2)- and AMP-activated protein kinase (AMPK) pathway. YPLP is orally active .
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- HY-160926
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Glutathione S-transferase
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Cancer
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16-Oxocafestol enhances levels of glutathione S-transferase (GST) and tissue sulfhydryl in liver and in small bowel mucosa .
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- HY-162408
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Protease Activated Receptor (PAR)
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Others
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PAR4 antagonist 3 (Compound 36) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 26.1 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 97.6 min .
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- HY-162409
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Protease Activated Receptor (PAR)
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Others
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PAR4 antagonist 4 (Compound 37) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 14.2 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 42.5 min .
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- HY-162485
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Dengue virus
Virus Protease
|
Infection
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DV-B-120 is a competitive inhibitor for dengue virus (DENV) with IC50s of 5.35, 7.39, 10.49 and 8.58 μM, for DENV-1, DENV-2, DENV-3 and DENV-4, respectively, by inhibiting NS2B-NS3 protease. DV-B-120 exhibits antiviral activity through inhibition of DENV replication .
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- HY-158365
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LRRK2
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Neurological Disease
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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 .
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- HY-161523
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Xanthine Oxidase
URAT1
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Metabolic Disease
|
XOR/URAT1-IN-1 (Compound II15) is a dual inhibitor for xanthine oxidoreductase (XOR) and uric acid transporter 1 (URAT1), with IC50 of 6 nM and 12.9 μM. XOR/URAT1-IN-1 lowers the levels of uric acid in Potassium oxonate (HY-17511)/Hypoxanthine (HY-N0091)-induced acute hyperuricemia mouse model .
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- HY-161723
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Dopamine Transporter
CDK
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Neurological Disease
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LH2-051 is a lysosome-enhancing lead compound, which promotes the lysosome biogenesis and the Aβ aggregate clearance through dopamine transporter-cyclin-dependent kinase 9-transcription factor EB (DAT-CDK9-TFEB) pathway. LH2-051 exhibits good pharmacokinetic characteristics in mouse models. LH2-051 is potential for ameliorating Aleheimer’s Disease .
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- HY-162407
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Btk
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Cancer
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I-As-1 is a potent inhibitor of Bruton’s tyrosine kinase (BTK), with the IC50 of 2.35 nM. I-As-1 shows antiproliferative activities among Ramos cells and OCI-LY10 cells with IC50s of 0.52 μM and 0.11 μM, respectively .
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- HY-146615
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TAM Receptor
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Cancer
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Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model .
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- HY-152031
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Amyloid-β
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Neurological Disease
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Glutaminyl Cyclase Inhibitor 5 (Compound 71) is a potent and selective human glutaminyl cyclase (hQC) inhibitor with an IC50 of 3.2 nM .
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- HY-W012977
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- HY-129246
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DNA/RNA Synthesis
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Cancer
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Cytembena is inhibitor for replicative DNA synthesis, purine synthesis and tetrahydrofolate formylase activity. Cytembena ameliorates ovarian or breast cancer, relieves the pain from skeletal metastases .
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- HY-161643
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Cholinesterase (ChE)
Keap1-Nrf2
|
Neurological Disease
Inflammation/Immunology
|
S21-1011 is a selective inhibitor for butyrylcholinesterase (BChE), with IC50 of 0.059 and 0.162 μM, for eqBChE and hBChE, respectively. S21-1011 exhibits good blood-brain barrier (BBB) permeability and good pharmacokinetic characters. S21-1011 exhibits anti-inflammatory activity through activation of keap1-Nrf2-ARE pathway (EC50 is 23.48 μM for antioxidant element ARE activation), ameliorates cognitive impairment in murine Alzheimer’s disease model .
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- HY-139414
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Interleukin Related
p38 MAPK
ERK
Apoptosis
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Inflammation/Immunology
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Lysophosphatidylcholines is an orally active lysolipid and a component of oxidized low density lipoprotein (LDL). Lysophosphatidylcholines induces cell injury, the production of IL-1β and apoptosis. Lysophosphatidylcholines has a proactive effect on sepsis .
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- HY-146619
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Amyloid-β
Serotonin Transporter
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Neurological Disease
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RAGE/SERT-IN-1 is a potent and orally active advanced glycation end products (RAGE) and serotonin transporter (SERT) inhibitor with IC50s of 8.26 μM and 31.09 nM, respectively. RAGE/SERT-IN-1 exhibits significant neuroprotective effect against Aβ25-35-induced neuronal damage and alleviates depressive behavior of mice. RAGE/SERT-IN-1 can be used for researching the comorbidity of Alzheimer's disease and depression .
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- HY-146883A
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Filovirus
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Infection
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As-358 (hydrochloride) has inhibitory effects against Ebola virus and Marburg virus with IC50s of 9.1 μM and 18.1 μM, as well as exhibits good in vivo safety .
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- HY-147943
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PROTACs
Btk
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Cancer
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PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth . PROTAC BTK Degrader-1 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-126383
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Bacterial
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Infection
Others
Inflammation/Immunology
Cancer
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Spilanthol is an orally active analgesic, neuroprotective, antioxidant, antimutagenic, anti-cancer, anti-inflammatory, antimicrobial and insecticidal compound.pilanthol can induce cAMP to inhibit negative regulation of urinary concentration mechanism. Spilanthol can be use as diuretic research .
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- HY-163505
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Bacterial
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Others
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Anti-MRSA agent 11 suppresses fluoroquinolone-sensitive strain USA500 and -resistant MRSA isolate Mu50 (MIC =0.39 μg/mL). Anti-MRSA agent 11 displayes favorable in vivo half-life and safety profiles .
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- HY-121152
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- HY-161627
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NF-κB
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Inflammation/Immunology
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Anemoside A3-methyl 6-aminohexanoate (Compound A3-6) is a derivative of Pulchinenoside C (Anemoside B4) (HY-N0205). Anemoside A3-methyl 6-aminohexanoate inhibits pyruvate carboxylase (PC) with an IC50 of 0.058 μM, reprograms macrophage function, and alleviates DSS-induced colitis through inhibition of the NF-κB and NLRP3 inflammasome pathway. Anemoside A3-methyl 6-aminohexanoate exhibits a moderate in vivo pharmacokinetic characters compared with Anemoside B4 .
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-
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- HY-126876
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Apoptosis
AMPK
Reactive Oxygen Species
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Cancer
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GL-V9 inhibits proliferation of HepG2 cell (IC50 is 35.2 μM) through induction of apoptosis and cell cycle arrest at G2/M phase. GL-V9 regulates mitochondrial membrane potential and increases the production of intracellular reactive oxygen species. GL-V9 inhibits the pentose phosphate pathway (PPP), enhances fatty acid oxidation (FAO) through activation of AMPK, and thus inhibits the metastasis of cancer cells. GL-V9 exhibits antitumor efficacy in mouse model .
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- HY-P10302A
-
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GLP Receptor
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Metabolic Disease
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GLP-1R/GIPR agonist-1 soduim is the sodium salt form of GLP-1R/GIPR agonist-1 (HY-P10302). GLP-1R/GIPR agonist-1 soduim is a dual agonist for glucagon-like peptide-1 receptor (GLP-1R, EC50 is 0.57 nM) and glucose-dependent insulin releasing peptide receptor (GIPR, EC50 is 0.75 nM). GLP-1R/GIPR agonist-1 soduim lowers blood sugar by mimicking the action of endogenous hormones GLP-1 and GIP, enhancing insulin secretion while inhibiting glucagon secretion. GLP-1R/GIPR agonist-1 soduim can be used in the study of metabolic diseases such as diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .
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- HY-143586
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CDK
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Cancer
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CDK7-IN-8 is a potent CDK7 inhibitor with IC50 of 54.29 nM. CDK7-IN-8 has inhibitory effect on certain cancer cells and in vivo tumor models .
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- HY-146468
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Dipeptidyl Peptidase
GPR119
Potassium Channel
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Metabolic Disease
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DPP-4/GPR119 modulator 1 (Compound 22) is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist. DPP-4/GPR119 modulator 1 shows blood glucose-lowering effect and moderate inhibition on hERG channel with an IC50 of 4.9 μM. DPP-4/GPR119 modulator 1 can be used for diabetes research . DPP-4/GPR119 modulator 1 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-162633
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Deubiquitinase
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Cancer
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USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC50 of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer .
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- HY-163345
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5-HT Receptor
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Neurological Disease
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5-HT7R antagonist 2 (compound 4h) is a 5-HT7R antagonist that antagonizes the G protein and β-arrestin signaling pathways, with a Ki of 67 nM, the IC50 values in cAMP and Tango tests were 2.59 μM and 39.57 μM, respectively. 5-HT7R antagonist 2 has an effect on neurogenesis and can reduce repetitive behaviors related to autism spectrum disorder (ASD) and restore neurogenesis of ASD impairment .
Pharmacokinetic Analysis ICR Male Mice
药代动力学分析
Plasma |
Intravenous Administration |
Intraperitoneal Administration |
Tmax (h) |
0.08 |
0.25 |
T1/2 (h) |
0.77 |
1.06 |
Cmax (ng/mL) |
33.07 |
156.44 |
AUClast (ng·h/mL) |
28.31 |
143.27 |
CL (L/h/kg) |
41.61 |
- |
Vss (L/kg) |
32.43 |
- |
MRT (h) |
0.79 |
0.93 |
F (%) |
50.60 |
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-
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- HY-115996
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Others
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Cancer
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Antitumor agent-51 possesses potent and selective inhibitory for osteosarcoma cell growth and migration with IC50 of 21.9 nM in MNNG/HOS cells. Antitumor agent-51 has a considerable bioavailability and a low toxicity .
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-
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- HY-145845
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HDAC
Monoamine Oxidase
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Neurological Disease
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HDAC1/MAO-B-IN-1 is a potent, selective and cross the blood-brain barrier HDAC1/MAO-B inhibitor with IC50 values of 21.4 nM and 99.0 nM for HDAC1 and MAO-B, respectively. HDAC1/MAO-B-IN-1 has the potential for the research of Alzheimer’s disease .
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- HY-158113
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Histone Acetyltransferase
PROTACs
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Cancer
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CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .
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- HY-146715
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Microtubule/Tubulin
Apoptosis
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Cancer
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IDO/Tubulin-IN-2 (HT2) is a potent TDO and tubulin inhibitor. IDO/Tubulin-IN-2 also shows potent activity against U87, HepG2, A549, HCT-116, and LO2 cancer cell lines, with IC50 values of 0.43, 0.036, 0.041, 0.095 and 1.04 μM, respectively. IDO/Tubulin-IN-2 remarkably promotes the antitumor activity .
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- HY-146672
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Itk
|
Cancer
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ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities .
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- HY-147395
-
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GPR52
|
Neurological Disease
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GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC50 value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity .
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- HY-143414
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Beta-lactamase
Bacterial
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Infection
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Metallo-β-lactamase-IN-6 is a potent VIM-Type metallo-β-lactamase inhibitor with IC50s of 0.56 μM, 29.50 μM and 5.78 μM for VIM-2, VIM-1 and VIM-5. Metallo-β-lactamase-IN-6 displays potent synergistic antibacterial activity with Meropenem against engineered Escherichia coli strains and intractable clinically isolated Pseudomonas aeruginosa producing VIM-2 MBL .
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-
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- HY-P10435
-
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Dopamine Receptor
|
Neurological Disease
|
KEMPFPKYPVEP is a 12-amino acids neuropeptide, which upregulates levels of dopamine (DA) and norepinephrine (NE) in the prefrontal cortex, exhibits spatial and object recognition memory promoting ability in Scopolamine (HY-N0296)-induced amnesia mouse model .
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-
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- HY-144658
-
|
Factor Xa
|
Cardiovascular Disease
|
FXIa-IN-8 is a potent and selective FXIa inhibitor with an IC50 of 14.2 nM. FXIa-IN-8 shows antithrombotic activity without increasing the bleeding risk and obvious toxicitysup>[1].
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-
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- HY-149844
-
|
Fungal
|
Infection
|
S-F24 is an antifungal agent with excellent broad-spectrum. S-F24 inhibits CYP3A4 with an IC50 value of 0.4 μM. S-F24 displays a good safety profile with high selectivity, low hemolytic effects, and low tendency to induce resistance. S-F24 can be used for research on fungal infections .
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- HY-160761
-
|
Opioid Receptor
|
Inflammation/Immunology
|
K-Opioid receptor agonist-1 (Compound 5a) is an agonist for κ-Opioid receptor with Ki of 0.25 nM and EC50 of 2 nM. K-Opioid receptor agonist-1 is blood brain barrier (BBB) penetrate (brain/plasma ratios of 0.50 to 0.65). K-Opioid receptor agonist-1 exhibits anti-inflammatory activity in dermatitis models induced by Arachidonic acid (HY-109590) or oxazolidinone .
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- HY-162600
-
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CDK
|
Inflammation/Immunology
|
CDK8-IN-15 (Compound 46) is a potent CDK8 inhibitors with an IC50 value of 57 nM. It can enhance the thermal stability of CDK8 along with inhibition against NF-κB and have favourable selectivity across the CDK family and tyrosine kinase. Additionally, it also demostrates a positive effect in vitro psoriasis model induced by TNF-α and alleviats the inflammatory response enhancing the expression of Foxp3 and IL-10, which is promising for research of psoriasis diseases .
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-
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- HY-143434
-
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FLT3
|
Cancer
|
FLT3/D835Y-IN-1 (compound 13a) is a orally active, potent and selective FLT3 and FLT3/D835Y inhibitor, with IC50 values of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 also blocks tumor growth, has anticancer efficacy, and can be used to research for AML (acute myeloid leukemia) .
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-
-
- HY-163403
-
|
VEGFR
|
Cardiovascular Disease
Cancer
|
VEGFR-2-IN-43 (compound 16) is an orally active inhibitor of VEGFR2, with an IC50 of 39.91 μM. VEGFR-2-IN-43 can be used for wet age-related macular degeneration (w-AMD) disease research .
|
-
Cat. No. |
Product Name |
Type |
-
- HY-139414
-
|
Biochemical Assay Reagents
|
Lysophosphatidylcholines is an orally active lysolipid and a component of oxidized low density lipoprotein (LDL). Lysophosphatidylcholines induces cell injury, the production of IL-1β and apoptosis. Lysophosphatidylcholines has a proactive effect on sepsis .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-163315
-
|
Keap1-Nrf2
AMPK
|
Metabolic Disease
|
YPLP is a yeast-derived peptide Tyr-Pro-Leu-Pro, which exhibits activity in anti fatigue mechanisms through the nuclear factor erythroid-2-related factor 2 (Nrf2)- and AMP-activated protein kinase (AMPK) pathway. YPLP is orally active .
|
-
- HY-P10302A
-
|
GLP Receptor
|
Metabolic Disease
|
GLP-1R/GIPR agonist-1 soduim is the sodium salt form of GLP-1R/GIPR agonist-1 (HY-P10302). GLP-1R/GIPR agonist-1 soduim is a dual agonist for glucagon-like peptide-1 receptor (GLP-1R, EC50 is 0.57 nM) and glucose-dependent insulin releasing peptide receptor (GIPR, EC50 is 0.75 nM). GLP-1R/GIPR agonist-1 soduim lowers blood sugar by mimicking the action of endogenous hormones GLP-1 and GIP, enhancing insulin secretion while inhibiting glucagon secretion. GLP-1R/GIPR agonist-1 soduim can be used in the study of metabolic diseases such as diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .
|
-
- HY-P10435
-
|
Dopamine Receptor
|
Neurological Disease
|
KEMPFPKYPVEP is a 12-amino acids neuropeptide, which upregulates levels of dopamine (DA) and norepinephrine (NE) in the prefrontal cortex, exhibits spatial and object recognition memory promoting ability in Scopolamine (HY-N0296)-induced amnesia mouse model .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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