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Phosphorylation Blocker

" in MedChemExpress (MCE) Product Catalog:

69

Inhibitors & Agonists

1

Screening Libraries

1

Fluorescent Dye

10

Peptides

2

Inhibitory Antibodies

8

Natural
Products

1

Isotope-Labeled Compounds

1

Click Chemistry

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-122198
    ML367

    		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 .
    ML367
  • HY-U00462
    D-Mannoheptulose

    		Others Metabolic Disease
    D-Mannoheptulose is a major non-structural carbohydrate in avocado. D-mannoheptulose is a specific inhibitor of D-glucose phosphorylation. D-Mannoheptulose can block insulin release and utilization of carbohydrate in rat .
    D-Mannoheptulose
  • HY-162092
    Multi-target Pt

    		NF-κB IKK Cancer
    Multi-target Pt (IV), an antitumor agent, suppresses the IKKβ phosphorylation, IκBα phosphorylation and NF-κB p65 phosphorylation and nuclear translocation, leading to blocked the NF-kB signal pathway .
    Multi-target Pt
  • HY-103471
    Y11

    		FAK Cancer
    Y11 inhibits FAK1 autophosphorylation by blocking phosphorylation of Y397 and decreases tumor growth .
    Y11
  • HY-120542
    SR 1824

    		PPAR Metabolic Disease
    SR 1824 is a non-agonist PPARγ ligand that blocks Cdk5-mediated phosphorylation. SR 1824 has anti-diabetic effects .
    SR 1824
  • HY-158178
    EGFR T790M/L858R-IN-7

    		EGFR Cancer
    EGFR T790M/L858R-IN-7 (Compound 72) is a novel pyrimidine compound that inhibits the EGFR T790M and L858R mutation with a high efficacy (93% inhibition rate at 0.05 μM). EGFR T790M/L858R-IN-7 functions by specifically binding to the kinase domain of EGFR, thereby inhibiting its phosphorylation activity .
    EGFR T790M/L858R-IN-7
  • HY-118922
    IW927

    		TNF Receptor Inflammation/Immunology
    IW927 is a potent small molecule antagonist that blocks the binding of TNF-α to TNFRc1 with an IC50 value of 50 nM and disrupts TNFα-induced IκB phosphorylation with an IC50 value of 600 nM .
    IW927
  • HY-108554
    Q94 hydrochloride

    		Protease Activated Receptor (PAR) Others
    Q94 hydrochloride, a selective PAR1 antagonist (IC50=916 nM), can selectively block PAR1/Gαq interaction and signalling. Q94 hydrochloride blocks PAR1-mediated increases in both CCL2 mRNA and protein levels in a dose-dependent manner. Q94 hydrochloride also completely blocks thrombin-induced ERK1/2 and MLC phosphorylation .
    Q94 hydrochloride
  • HY-N1987
    Cucurbitacin IIb
    1 Publications Verification

    		 Apoptosis Inflammation/Immunology
    Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α .
    Cucurbitacin IIb
  • HY-N6782
    Oligomycin
    Maximum Cited Publications
    34 Publications Verification

    		 Oxidative Phosphorylation ATP Synthase Fungal Antibiotic Infection Cancer
    Oligomycin, an antifungal antibiotic, is an inhibitor of H +-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells .
    Oligomycin
  • HY-107593
    PS-1145 dihydrochloride

    		IKK Inflammation/Immunology
    PS-1145 (dihydrochloride) is a potent IκB kinase-2 inhibitor with an IC50 value of 88 nM. PS-1145 (dihydrochloride) inhibits activity of NF-κB by blocking IκB kinase phosphorylation in tumor-bearing rats .
    PS-1145 dihydrochloride
  • HY-110335
    OXA-06 hydrochloride

    		ROCK Cancer
    OXA-06 hydrochloride is an ATP-competitive ROCK inhibitor that blocks anchorage-dependent growth and invasion of non-small cell lung cancer cell lines. OXA-06 hydrochloride inhibits cofilin phosphorylation but does not stimulate apoptosis .
    OXA-06 hydrochloride
  • HY-118052
    BPKDi

    		PKD Cardiovascular Disease
    BPKDi is a potent bipyridyl PKD inhibitor with IC50s of 1 nM, 9 nM and 1 nM for PKD1, PKD2 and PKD3, respectively. BPKDi blocks signal-dependent phosphorylation and nuclear export of class IIa HDACs in cardiomyocytes .
    BPKDi
  • HY-U00462S
    D-Mannoheptulose-13C

    		Isotope-Labeled Compounds Metabolic Disease
    D-Mannoheptulose- 13C is the 13C labeled D-Mannoheptulose. D-Mannoheptulose is a major non-structural carbohydrate in avocado. D-mannoheptulose is a specific inhibitor of D-glucose phosphorylation. D-Mannoheptulose can block insulin release and utilization
    D-Mannoheptulose-13C
  • HY-163432
    YGL-12

    		PPAR Metabolic Disease
    YGL-12 is a potent PPARγ modulator with good binding affinity and an IC50 value of 0.85 μM. YGL-12 effectively blocks PPARγ Ser273 phosphorylation and can be used in diabetes research .
    YGL-12
  • HY-150700
    RLX-33

    		ERK Metabolic Disease
    RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome .
    RLX-33
  • HY-12960
    SKLB4771

    FLT3-​IN-​1

    		 FLT3 c-Kit Apoptosis Cancer
    SKLB4771 is a potent and selective Flt3 inhibitor with an IC50 value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue .
    SKLB4771
  • HY-P3695
    VSPPLTLGQLLS

    		FGFR Cancer
    VSPPLTLGQLLS is a small peptide FGFR3 inhibitor, peptide P3, inhibits FGFR3 phosphorylation. VSPPLTLGQLLS inhibits 9-cisRA-induced tracheal lymphangiogenesis and blocks lymphatic endothelial cell (LEC) proliferation, migration, and tubule formation .
    VSPPLTLGQLLS
  • HY-P10359
    TAT-QFNP12

    		TGF-beta/Smad MMP Neurological Disease
    TAT-QFNP12 block the NDRG2-PPM1A binding and reduce Smad2/3 phosphorylation, decreased astrocytic MMP-9 production and BBB disruption after subarachnoid hemorrhage (SAH) .
    TAT-QFNP12
  • HY-P3695A
    VSPPLTLGQLLS TFA

    		FGFR Cancer
    VSPPLTLGQLLS TFA is a small peptide FGFR3 inhibitor, peptide P3, inhibits FGFR3 phosphorylation. VSPPLTLGQLLS TFA inhibits 9-cisRA-induced tracheal lymphangiogenesis and blocks lymphatic endothelial cell (LEC) proliferation, migration, and tubule formation .
    VSPPLTLGQLLS TFA
  • HY-151776
    Cy3 methyltetrazine

    TZ-Cy3

    		 Fluorescent Dye Others
    Cy3 methyltetrazine (TZ-Cy3) is a click chemistry reagent with methyltetrazine building blocks that is highly reactive towards cyclooctene. Cy3 methyltetrazine is also a tetrazine-modified fluorescent probe that can be used to analyze protein phosphorylation in solution and living cells .
    Cy3 methyltetrazine
  • HY-108559
    L-161982

    		Prostaglandin Receptor Inflammation/Immunology
    L-161982 is a selective EP4 receptor antagonist. L-161982 completely blocks PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 alleviates collagen-induced arthritis in mice .
    L-161982
  • HY-P2282
    APTSTAT3-9R
    1 Publications Verification

    		 STAT Cancer
    APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity .
    APTSTAT3-9R
  • HY-15597
    Salinomycin
    25+ Cited Publications

    Procoxacin

    		 Bacterial Wnt β-catenin Mitophagy Autophagy Apoptosis Antibiotic Parasite Cancer
    Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, selectively inhibits the growth of gram-positive bacteria. Salinomycin is a potent inhibitor of Wnt/β-catenin signaling, blocks Wnt-induced LRP6 phosphorylation. Salinomycin (Procoxacin) shows selective activity against human cancer stem cells .
    Salinomycin
  • HY-139833
    Anti-inflammatory agent 6

    		NF-κB IKK Inflammation/Immunology
    Anti-inflammatory agent 6 blocks the phosphorylation of I kappa b kinase α/β (IKKα/β), IκBα, and nuclear factor kB p65 (NF-κB p65) which is a key controller of inflammation, thereby showing anti-inflammatory potential.
    Anti-inflammatory agent 6
  • HY-N0811
    Anemarsaponin B

    		NO Synthase COX NF-κB MEK Inflammation/Immunology
    Anemarsaponin B is a steroidal saponin. Anemarsaponin B decreases the protein and mRNA levels of iNOS and COX-2. Anemarsaponin B reduces the expressions and productions of pro-inflammatory cytokines, including TNF-a and IL-6. Anemarsaponin B inhibits the nuclear translocation of the p65 subunit of NF-κB by blocking the phosphorylation of IκBα. Anemarsaponin B also inhibits the phosphorylation of MAP kinase kinases 3/6 (MKK3/6) and mixed lineage kinase 3 (MLK3). Anti-inflammatory effect .
    Anemarsaponin B
  • HY-18758
    IN-1130
    1 Publications Verification

    		 TGF-β Receptor Inflammation/Immunology Cancer
    IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis .
    IN-1130
  • HY-17439
    Salinomycin sodium salt
    25+ Cited Publications

    Salinomycin sodium; Sodium salinomycin

    		 Wnt β-catenin Bacterial Autophagy Apoptosis Antibiotic Parasite Cancer
    Salinomycin sodium salt (Salinomycin sodium), an antibiotic potassium ionophore, is a potent inhibitor of Wnt/β-catenin signaling. Salinomycin sodium salt (Salinomycin sodium) acts on the Wnt/Fzd/LRP complex, blocks Wnt-induced LRP6 phosphorylation, and causes degradation of the LRP6 protein. Salinomycin sodium salt (Salinomycin sodium) shows selective activity against human cancer stem cells .
    Salinomycin sodium salt
  • HY-112700
    SHIP2-IN-1

    		Phosphatase Neurological Disease
    SHIP2-IN-1 is a potent SHIP2 inhibitor, inhibits SHIP2 activity, with an IC50 of 2 µM. SHIP2-IN-1 blocks GSK3β activation by phosphorylation at the Ser9 residue. SHIP2-IN-1 is used in the research of Alzheimer’s disease .
    SHIP2-IN-1
  • HY-110198
    ONO-8130

    		Prostaglandin Receptor PERK Inflammation/Immunology
    ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research .
    ONO-8130
  • HY-147905
    CDK9-IN-18

    		CDK Apoptosis Cancer
    CDK9-IN-18 is a potent CDK9 inhibitor. CDK9-IN-18 blocks the phosphorylation function of kinase CDK9. CDK9-IN-18 exhibits both good anticancer activity and low cellular activity. CDK9-IN-18 induces apoptosis.
    CDK9-IN-18
  • HY-136882
    TM-1

    		PDHK Cancer
    TM-1 is a potent inhibitor of pyruvate dehydrogenase kinase (PDHK1). TM-1 inhibits PDHK1 and PDHK2 with IC50s of 2.97 μM and 5.2 μM, respectively. TM-1 blocks pyruvate dehydrogenase complex (PDHC) phosphorylation, and inhibits cell proliferation .
    TM-1
  • HY-155554
    SCAL-255

    		Oxidative Phosphorylation Mitochondrial Metabolism Cancer
    SCAL-255 is a potent mitochondrial complex I (CI) inhibitor with IC50 of 1.14 μM. SCAL-255 blocks mitochondrial function, inhibits OCR, induces ROS production, and reduces MMP. SCAL-255 displays a considerable antiproliferation effect against oxidative phosphorylation (OXPHOS)-dependent cancer cells .
    SCAL-255
  • HY-155555
    SCAL-266

    		Oxidative Phosphorylation Mitochondrial Metabolism Cancer
    SCAL-266 is a potent mitochondrial complex I (CI) inhibitor with IC50 of 0.83 μM. SCAL-266 blocks mitochondrial function, inhibits OCR, induces ROS production, and reduces MMP. SCAL-266 displays a considerable antiproliferation effect against oxidative phosphorylation (OXPHOS)-dependent cancer cells .
    SCAL-266
  • HY-12283
    Rostafuroxin
    1 Publications Verification

    PST 2238

    		 Na+/K+ ATPase RSV Cardiovascular Disease
    Rostafuroxin (PST 2238), a digitoxigenin derivative, is an orally active and potent Na +,K +-ATPase (ATP1A1) antognist. Rostafuroxin binds specifically to the ATP1A1 extracellular domain and blocks respiratory syncytial virus (RSV)-triggered EGFR Tyr845 phosphorylation. Rostafuroxin has antihypertensive and anti-RSV activity .
    Rostafuroxin
  • HY-155805
    CAF-382

    		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 .
    CAF-382
  • HY-144043
    ALK5-IN-8

    		TGF-β Receptor Cancer
    ALK5-IN-8 is a potent inhibitor of TGFβRI (ALK5). ALK5-IN-8 Inhibits the phosphorylation of ALK5 on its downstream signaling proteins (Smad2 or Smad3) by blocking the binding of TGFβRI to ligands, thereby affecting or blocking TGF-β signaling. ALK5-IN-8 has the potential for the research of various ALK5-mediated related diseases (extracted from patent WO2021190425A1, compound 1) .
    ALK5-IN-8
  • HY-P99161
    Tilvestamab

    BGB149

    		 TAM Receptor Cancer
    Tilvestamab (BGB149) is a humanized anti-AXL antibody that blocks AXL-mediated cell signaling. Tilvestamab significantly inhibits Gas6-induced AXL activation in 786-0-Luc RCC cells and inhibits downstream AKT phosphorylation. Tilvestamab can be used in cancer research, particularly in AXL overexpressing renal cell carcinomas .
    Tilvestamab
  • HY-149143
    JNJ-28583113

    		TRP Channel Inflammation/Immunology
    JNJ-28583113 is an TRPM2 antagonist with brain permeability. JNJ-28583113 inhibits TRPM2 blocked phosphorylation of GSK3α and β subunits. JNJ-28583113 protects cells from oxidative stress induced cell death. JNJ-28583113 also suppresses cytokine release in response to pro-inflammatory stimuli in microglia .
    JNJ-28583113
  • HY-162317
    AMPK-IN-5

    		JAK p38 MAPK Infection
    AMPK-IN-5 (compound 7m) is a Osthole (HY-N0054) derivative, and blocks MAPK signal transduction by inhibiting the phosphorylation of JNK and p38, thereby inhibiting the release of inflammatory cytokines. AMPK-IN-5 reduce DSS-induced ulcerative colitis and LPS (HY-D1056)-induced acute lung injury .
    AMPK-IN-5
  • HY-12274
    ML347
    5 Publications Verification

    LDN 193719

    		 TGF-β Receptor Cancer
    ML347 (LDN193719) is a highly selective ALK1/ALK2 inhibitor. ML347 has IC50 values of 46 and 32 nM against ALK1 and ALK2, respectively, >300-fold selective over ALK3. ML347 block the phosphorylation of Smad1/5 by TGF-β1 .
    ML347
  • HY-144321
    Trk-IN-9

    		Trk Receptor Cancer
    Trk-IN-9 (Compound 12) is a potent inhibitor of TRK. Trk-IN-9 inhibits the proliferation of Km-12 cell lines. Trk-IN-9 induces the apoptosis of Km-12 cells in a concentration-dependent manner. Trk-IN-9 inhibits the phosphorylation of TRK to block downstream pathways. Trk-IN-9 has the potential for the research of NTRK-fusion cancers .
    Trk-IN-9
  • HY-107595
    SD-1008

    		JAK STAT Apoptosis Cancer
    SD-1008 is a potent JAK inhibitor. SD-1008 inhibits tyrosyl phosphorylation of STAT3, JAK2 and Src. SD-1008 also reduces STAT3-dependent luciferase activity. SD-1008 enhances apoptosis induced by Paclitaxel in ovarian cancer cells via directly blocking the JAK-STAT3 signaling pathway .
    SD-1008
  • HY-112701
    CCR6 inhibitor 1
    5 Publications Verification

    		 CCR Inflammation/Immunology Endocrinology Cancer
    CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, with IC50s of 0.45 and 6 nM for monkey and human CCR6, much more selective at CCR6 over human CCR1 (IC50, > 30000 nM), and CCR7 (IC50, 9400 nM). CCR6 inhibitor 1 markedly blocks ERK phosphorylation. CCR6 inhibitor 1 is used in the research of autoimmune diseases and cancer .
    CCR6 inhibitor 1
  • HY-N6064
    Polygalacin D
    1 Publications Verification

    		 Apoptosis IAP Cancer
    Polygalacin D (PGD) is a bioactive compound isolated from Platycodon grandiflorum with anticancer and anti-proliferative properties. PGD suppresses the expression of the IAP family of proteins including survivin, cIAP-1 and cIAP-2 and blocks the PI3K/Akt pathway by inhibiting the phosphorylation of GSK3β, Akt and the expression of PI3K. Polygalacin D induces apoptosis
    Polygalacin D
  • HY-P10465
    TRPV1-Tat

    		TRP Channel Inflammation/Immunology
    TRPV1-Tat is an antagonistic peptide that fuses the TRPV1 (transient receptor potential vanilla subtype 1) of the cell-penetrating peptide Tat. TRPV1-Tat blocks this phosphorylation process by competitively binding to the AKAP79 binding site of TRPV1, thereby inhibiting the sensitization of TRPV1. TRPV1-Tat can be used in the study of inflammatory pain .
    TRPV1-Tat
  • HY-103248
    Toyocamycin
    4 Publications Verification

    Vengicide

    		 IRE1 Fungal Antibiotic Apoptosis CDK Infection Cancer
    Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC50 value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC50 value of 79 nM .
    Toyocamycin
  • HY-116753
    (-)Clausenamide

    		Amyloid-β Tau Protein Neurological Disease
    (-)Clausenamide is an active alkaloid isolated from the leaves of Clausena lansium (Lour.) Skeels, and improves cognitive function in both normal physiological and pathological conditions. (-)Clausenamide inhibits β-amyloid (Aβ) toxicity, blocking neurofibrillary tangle formation by inhibiting the phosphorylation of tau protein. (-)Clausenamide exerts a significant neuroprotective activity against Aβ25-35. (-)Clausenamide can be used for researching Alzheimer's disease (AD) .
    (-)Clausenamide
  • HY-150582
    c-Met-IN-14

    		c-Met/HGFR c-Kit FLT3 Apoptosis Cancer
    c-Met-IN-14 (compound 26af) is a selective inhibitor of c-Met kinase from N-sulfonylamidine-based derivatives, with an IC50 value of 2.89 nM. c-Met-IN-14 shows anticancer activity by blocking phosphorylation of c-Met, and arrests cell cycle at G2/M phase. c-Met-IN-14 induces apoptosis of A549 cells in a dose-dependent manner .
    c-Met-IN-14
  • HY-156618
    Irpagratinib

    ABSK011

    		 FGFR Cancer
    Irpagratinib (ABSK011) is an orally active inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinase, targeting to FGFR4 (IC50<10 nM). Irpagratinib inhibits the auto-phosphorylation of FGFR4 and blocks signal transduction from FGFR4 to downstream pathway activation. Irpagratinib exhibits high exposure in PK study in mouse, rat and dog, and also shows antineoplastic/anti-tumor activity in subcutaneous xenograft tumor models .
    Irpagratinib

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