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Kinase inhibition

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158

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1

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9

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16

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-162255

    CDK Cancer
    CDK2-IN-23 (Compound 17) is a kinase selective and highly potent CDK2 inhibitor (IC50 = 0.29 nM). CDK2-IN-23 shows the pharmacodynamic inhibition of CDK2 in CCNE1-amplified mouse models. CDK2-IN-23 can be used for the research of cancer .
    CDK2-IN-23
  • HY-148314

    ROS Kinase Cancer
    ROS kinases-IN-2 is a ROS kinase inhibitor with 21.53% inhibition at 10 μM .
    ROS kinases-IN-2
  • HY-15979
    H-89
    Maximum Cited Publications
    124 Publications Verification

    PKA Autophagy Neurological Disease
    H-89 is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase, and others kinases.
    H-89
  • HY-15979A
    H-89 dihydrochloride
    Maximum Cited Publications
    124 Publications Verification

    PKA Autophagy Others
    H-89 dihydrochloride is a potent and selective inhibitor of protein kinase A (PKA) with an IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase.
    H-89 dihydrochloride
  • HY-P1479A

    Autophagy CaMK Neurological Disease
    Calmodulin-Dependent Protein Kinase II (290-309) acetate is a potent CaMK antagonist with an IC50 of 52 nM for inhibition of Ca2+/calmodulin-dependent protein kinase II .
    Calmodulin-Dependent Protein Kinase II(290-309) acetate
  • HY-144706

    TAM Receptor Cancer
    Axl-IN-3 is a potent, selective and orally active AXL kinase inhibitor with an IC50 of 41.5 nM. Axl-IN-3 has lower inhibition of other kinases .
    Axl-IN-3
  • HY-P1479

    Autophagy CaMK Neurological Disease
    Calmodulin-Dependent Protein Kinase II (290-309) is a potent CaMK antagonist with an IC50 of 52 nM for inhibition of Ca2+/calmodulin-dependent protein kinase II .
    Calmodulin-Dependent Protein Kinase II (290-309)
  • HY-P3841

    PKC Others
    Protein Kinase C β Peptide is a peptide fragment of Protein Kinase Cβ. Protein Kinase Cβ is related with hyperglycemia decreases endothelium-derived nitric oxide. Inhibition of Protein kinase Cβ prevents the reduction in endothelium-dependent vasodilation induced by acute hyperglycemia .
    Protein Kinase C β Peptide
  • HY-N3702

    Syk Inflammation/Immunology
    Dehydroabietinol is an abietane diterpenoid. Dehydroabietinol has kinase inhibition activity for spleen tyrosine kinase (SYK) with an IC50 value of 46.4 μM. Dehydroabietinol can be used for the research of immune-mediated disease .
    Dehydroabietinol
  • HY-171252

    EGFR Cancer
    EGFR-IN-145 (compound 7c) is an EGFR kinase inhibitor. At a concentration of 20 μM, EGFR-IN-145 has an inhibition rate of 52.7% on EGFR-wild type kinase .
    EGFR-IN-145
  • HY-141864

    Itk Inflammation/Immunology
    ITK/TRKA-IN-1 is a dual inhibitor of IL-2-inducible T-cell kinase (ITK) and tropomyosin receptor kinase A (TRKA) with an IC50 value of 1.0 nM and 96 % inhibition, respectively.
    ITK/TRKA-IN-1
  • HY-116529

    Others Others
    Lamellarin E is a biologically active marine alkaloid, while the Lamellarin series of alkaloids show potential cytotoxicity, topoisomerase I inhibition, protein kinase inhibition, multidrug resistance reversal, and anti-HIV-1 activity .
    Lamellarin E
  • HY-148112

    Casein Kinase Neurological Disease
    Casein kinase 1δ-IN-1 (compound 822) is an inhibitor of casein kinase 1 delta (CK1δ), exhibits inhibition of greater than 5%. Casein kinase 1δ-IN-1 can be used for neurodegenerative disorders such as Alzheimer's disease research .
    Casein kinase 1δ-IN-1
  • HY-B1898

    PKA Metabolic Disease
    Metadoxine blocks adipocyte differentiation in association with inhibition of the protein kinase A-cAMP response element binding protein (PKA-CREB) pathway.
    Metadoxine
  • HY-49073

    p38 MAPK Cancer
    p38 MAP Kinase Inhibitor VI (compound c32) is a p38 MAPK inhibitor with an inhibition rate of 24% .
    p38 MAP Kinase Inhibitor Ⅵ
  • HY-15802
    WZ4003
    5 Publications Verification

    AMPK Cancer
    WZ4003 is the first potent and highly specific NUAK kinase inhibitor with IC50 of 20 nM/100 nM for NUAK1 (ARK5)/NUAK2, without significant inhibition on other 139 kinases.
    WZ4003
  • HY-112266

    MARK AMPK Neurological Disease
    MARK-IN-4 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of 1 nM. Inhibition of microtubule affinity regulating kinase (MARK) represents a potentially attractive means of arresting neurofibrillary tangle pathology in Alzheimer's disease .
    MARK-IN-4
  • HY-150027

    VEGFR PDGFR Cancer
    Multi-kinase-IN-3 (compound 2) is a potent angiokinase inhibitor. Multi-kinase-IN-3 shows inhibition activity against VEGFR-2 and PDGFRβ, with IC50 values of 58.3 and 55 nM, respectively .
    Multi-kinase-IN-3
  • HY-164041

    PKC Others
    Staurosporine-Boc, a natural product isolated from the actinomyces Streptomyces staurosporeus, is a potent non-selective inhibitor of protein kinase. Staurosporine-Boc inhibits a variety of protein kinases, including protein kinase C (PKC), tyrosine kinase, and serine/threonine kinase. Because of its broad inhibition profile, Staurosporine-Boc is widely used as a tool compound in biological research, especially when studying cell signaling pathways .
    Staurosporine-Boc
  • HY-112082

    ERK Cancer
    BAY885 is a highly potent and selective ERK5 inhibitor with an IC50 of 35 nM. BAY885 shows weak inhibition on others kinases .
    BAY885
  • HY-149075

    Salt-inducible Kinase (SIK) Cancer
    MR22 is a potent pan-SIK (salt-inducible kinase) inhibitor. MR22 no longer exhibits activity on STE group kinases and displays excellent selectivity in a representative kinase panel. MR22-dependent SIK inhibition led to centrosome dissociation and subsequent cell-cycle arrest in ovarian cancer cells .
    MR22
  • HY-144381

    Bacterial Infection
    Glutamate-5-kinase-IN-1 (compound 50) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.1 µM. Glutamate-5-kinase-IN-1 shows G5K inhibition by alters the ATP binding site architecture for enzyme recognition. Glutamate-5-kinase-IN-1 has the potential for the research of anti-TB agents .
    Glutamate-5-kinase-IN-1
  • HY-144382

    Bacterial Infection
    Glutamate-5-kinase-IN-2 (compound 54) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.2 µM. Glutamate-5-kinase-IN-2 shows G5K inhibition by promotes conformational changes at the L-glutamate binding site. Glutamate-5-kinase-IN-2 has the potential for the research of anti-TB agents .
    Glutamate-5-kinase-IN-2
  • HY-149415

    RET FGFR VEGFR c-Kit c-Met/HGFR PDGFR Raf Cancer
    Multi-kinase-IN-5 (compound 15c) is a promising multi-kinase inhibitory agent. Multi-kinase-IN-5 inhibits a panel of protein kinases (RET, KIT, cMet, VEGFR1,2, FGFR1, PDGFR and BRAF), showing % inhibition of 74%, 31%, 62%, 40%, 73%, 74%, 59%, and 69%, respectively, and IC50 of 1.287, 0.117 and 1.185 μM against FGFR1, VEGFR, and RET kinases, respectively .
    Multi-kinase-IN-5
  • HY-141896

    RET Cancer
    RET-IN-7 demonstrates potent in vitro RET kinase inhibition and robust in vivo efficacy in RET-driven tumor xenografts upon multiday dosing in mice.
    RET-IN-7
  • HY-15814

    Bcr-Abl PDGFR c-Kit Src JAK Apoptosis Cancer
    HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression .
    HG-7-85-01
  • HY-160708

    Tie Cancer
    Tie2 kinase inhibitor 3 (compound 63) is a potent Tie-2 kinase inhibitor with good oral activity (IC50=30 nM). Tie2 kinase inhibitor 3 inhibits phosphorylation and signaling of Tie-2 by competing with the ATP binding site of Tie-2 kinase. This inhibition affects the stability and maturity of blood vessels, which has an impact on tumor angiogenesis. Tie2 kinase inhibitor 3 can be used to restrict tumor growth and regulate angiogenesis .
    Tie2 kinase inhibitor 3
  • HY-P10346

    Smooth-Muscle Myosin Light-Chain Kinase (796-815)

    Myosin Cardiovascular Disease Inflammation/Immunology
    smMLCK peptide is a specific inhibitor of smooth muscle myosin light chain kinase (smMLCK). The smMLCK peptide mimics the substrate and competitively inhibits the binding of the actual substrate to the enzyme, thereby inhibiting the kinase activity. This inhibition prevents the phosphorylation of the myosin light chain, thus inhibiting muscle contraction .
    smMLCK peptide
  • HY-125068

    Cytochrome P450 p38 MAPK Inflammation/Immunology
    RPR203494 is a potent inhibitor against CYP isozymes. RPR203494 shows inhibition against p38 kinase with an IC50 value of 9 nM and an EC50 value of 60 nM. RPR203494 demonstrates an inhibition of hepatic Cytochrome P450. RPR203494 is promising for research of rheumatoid arthritis (RA) .
    RPR203494
  • HY-132808

    SAR 444727; PRN473

    Btk Inflammation/Immunology
    Atuzabrutinib (SAR 444727) is a potent, selective reversible inhibitor of Btk (Bruton's tyrosine kinase) inhibitor. Atuzabrutinib inhibits neutrophil recruitment via inhibition of macrophage antigen-1 signalling .
    Atuzabrutinib
  • HY-164413

    VEGFR EGFR RET Apoptosis Cancer
    CLM3, a pyrazolopyrimidine derivative, is a multiple tyrosine kinase inhibitor. CLM3 shows antiproliferative and proapoptotic activity on endothelial and cancer cells, synergistically enhanced by SN38 (HY-13704). These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, EGFR and RET tyrosine kinases and their related signaling pathways .
    CLM3
  • HY-12461

    PI3K EGFR GABA Receptor FLT3 IKK Neurological Disease Metabolic Disease Inflammation/Immunology
    WS6 is an IkB kinase and EBP1 inhibitor, with IC50 values of 0.24 nM, 0.21 nM, and 40.48 nM in MV4-11, MOLM13, and K562 cells, respectively. WS6 promotes the proliferation of alpha and beta cells in the pancreas, has antioxidant and anti-inflammatory activities, and can alleviate depression like behavior in rats [1][2][4].
    WS6
  • HY-12299
    WH-4-023
    4 Publications Verification

    Dual LCK/SRC inhibitor

    Src Cancer
    WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.
    WH-4-023
  • HY-10966
    SB-590885
    5+ Cited Publications

    Raf Cancer
    SB-590885 is a potent?B-Raf?inhibitor with?Ki?of 0.16 nM, and has 11-fold greater selectivity for B-Raf over c-Raf, without inhibition to other human kinases.
    SB-590885
  • HY-125762

    Tyrosinase Cancer
    Tyrosinase-IN-16 (compound 19a) is a tyrosine kinase (Tyrosinase) inhibitor with Ki=470 nM. Tyrosinase-IN-16 is cytotoxic to B16F10 cells, with >90% inhibition at 20 μM .
    Tyrosinase-IN-16
  • HY-144687

    ATM/ATR PI3K mTOR Cancer
    ATM Inhibitor-4 (compound 39) is a potent and selective ATM inhibitor, with an IC50 of 0.32 nM. ATM Inhibitor-4 shows stronger inhibition of PI3K kinases family. ATM Inhibitor-4 shows a full inhibition of mTOR at 1 μM. ATM Inhibitor-4 exhibits favorable metabolic stability .
    ATM Inhibitor-4
  • HY-12900

    SphK Inflammation/Immunology Cancer
    RB-005 is a selective inhibitor of sphingosine kinase 1 (SK1) (IC50=3.6 µM), with weaker inhibition of another isoenzyme, SK2. The selective inhibition of RB-005 helps to distinguish the biological functions and roles of SK1 and SK2, which can be used in the study of inflammatory diseases and cancer .
    RB-005
  • HY-N2484

    Astrapterocarpan

    PDGFR ERK Cardiovascular Disease
    Methylnissolin (Astrapterocarpan), isolated from Astragalus membranaceus, inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC50 of 10 μM. Methylnissolin inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERIC1/2) mitogen-activated protein (MAP) kinase. Methylnissolin inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibition of the ERK1/2 MAP kinase cascade .
    Methylnissolin
  • HY-147695

    c-Met/HGFR Cancer
    c-Met-IN-12 (compound 4r) is an orally active, potent and selective type II c-Met kinase inhibitor, with an IC50 of 10.6 nM. c-Met-IN-12 displays high inhibitory effects (inhibition rate > 80% in 1 μM) against AXL, Mer and TYRO3 kinases. c-Met-IN-12 can be used a scaffold for further kinase selectivity enhancement. c-Met-IN-12 shows antitumor efficacy .
    c-Met-IN-12
  • HY-15798

    VSV TAM Receptor Cardiovascular Disease
    UNC2881 is an orally active and specific Mer kinase inhibitor, inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM. UNC2881 shows additional inhibition against Axl and Tyro with IC50s of 360 nM and 250 nM, respectively. UNC2881 potently inhibits collagen-induced platelet aggregation, can be used for pathologic thrombosis research .
    UNC2881
  • HY-W110242A

    Endogenous Metabolite Cardiovascular Disease
    (S)-CPP sodium serves as an inhibitor of the branched-chain α-ketoacid dehydrogenase complex (BCKDC) kinase, commonly referred to as BDK or keto acid dehydrogenase kinase. As a negative regulator of BCKDC activity, the inhibition of BDK by (S)-CPP (with an IC50 of 6.3 μM) results in the activation of the complex and a notable decrease in plasma levels of leucine/isoleucine and valine in wild-type mice.
    (S)-CPP sodium
  • HY-121998

    Aurora Kinase Others
    Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki=0.36 μM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division when used at a concentration of 40 μM but does not affect ring ingression, suggesting that Aurora B kinase activity is not required for that step.
    Binucleine 2
  • HY-P1597
    Malantide
    1 Publications Verification

    PKA PKC Cancer
    Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide is also an efficient substrate for PKC with a Km of 16 μM .
    Malantide
  • HY-112400

    BIM V

    Ribosomal S6 Kinase (RSK) Cancer
    Bisindolylmaleimide V is a cell-permeable negative control for protein kinase C inhibition studies with an IC50 value over 100 µM . Bisindolylmaleimide V blocks the activation of mitogen-stimulated protein kinase p70 s6k/p85 s6k (S6K) in vivo with an IC50 of 8 µM .
    Bisindolylmaleimide V
  • HY-108431

    Apoptosis Cancer
    MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis. MN58b reduces cell growth through the induction of apoptosis, and also has antitumoral activity .
    MN58b
  • HY-150561

    Trk Receptor Cancer
    Trk-IN-20 is a kind of 3-vinylindazole derivatives. Trk-IN-20 suppresses Trk kinases functions by phosphorylation inhibition of TrkA/B/C with IC50 values of 1.6 nM, 2.9 nM and 2.0 nM, respectively .
    Trk-IN-20
  • HY-12037A
    Rigosertib
    5 Publications Verification

    ON-01910

    Polo-like Kinase (PLK) PI3K Apoptosis Cancer
    Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
    Rigosertib
  • HY-P1597A

    PKA PKC Cancer
    Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide TFA is also an efficient substrate for PKC with a Km of 16 μM .
    Malantide TFA
  • HY-164840

    Clofarabine-TP

    DNA/RNA Synthesis Cancer
    Clofarabine-5'-triphosphate is the metabolite of Clofarabine (HY-A0005) by deoxycytidine kinase (dCK) phosphorylation. Clofarabine-5'-triphosphate exhibits cytotoxicity in cancer cells through inhibition of DNA synthesis and DNA repair .
    Clofarabine-5'-triphosphate
  • HY-169231

    Bcr-Abl Cancer
    BCR-ABL-IN-10 (compound B4) is a covalent and aryl vinyl sulfate (AVS)-containing BCR-ABL inhibitor with an IC50 of 43.1 nM for ABL kinase. BCR-ABL-IN-10 forms a covalent and stable adduct with ABL kinase, leading to sustained inhibition of endogenous BCR-ABL activities. BCR-ABL-IN-10 can be used for the study of chronic myeloid leukemia (CML) .
    BCR-ABL-IN-10

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