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FAK inhibitor

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81

Inhibitors & Agonists

1

Biochemical Assay Reagents

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9

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-128580
    FAK inhibitor 2
    1 Publications Verification

    FAK Cancer
    FAK inhibitor 2 is a potent focal adhesion kinase (FAK) inhibitor with an IC50  of 0.07 nM, with antitumor and anti-angiogenesis activities .
    <em>FAK</em> <em>inhibitor</em> 2
  • HY-12444
    Y15
    15+ Cited Publications

    FAK inhibitor 14

    FAK Cancer
    Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.
    Y15
  • HY-18928

    FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range .
    <em>FAK</em> <em>inhibitor</em> 5
  • HY-146203

    FAK Cancer
    Compound 26F not only optimized the effective inhibitory enzyme (ic50= 28.2 nm), but also showed relatively less cytotoxicity (ic50= 3.32 μ M) And induced MDA-MB-231 cell apoptosis in a dose-dependent manner, effectively blocking MDA-MB-231 cells in g0/g1 phase.
    <em>FAK</em> <em>inhibitor</em> 6
  • HY-157553

    FAK Cancer
    FAK-IN-19 (ligand3) is an inhibitor in a co-crystal structure with FAK. FAK-IN-19 has anticancer effects .
    FAK-IN-19
  • HY-155440

    FAK Cancer
    FAK-IN-15 (Compound 9b) is a focal adhesion kinase (FAK) inhibitor with an IC50 value of 0.2691 nM. FAK-IN-15 has anti-tumor activity with an IC50 value of 1.033 μM against U87-MG cells .
    FAK-IN-15
  • HY-155439

    FAK Cancer
    FAK-IN-14 (compound 8d) is a focal adhesion kinase(FAK) inhibitor with an IC50 value of 0.2438 nM. FAK-IN-14 induces U87-MG cell early apoptosis and arrest the cell at the G2/M phase .
    FAK-IN-14
  • HY-144448

    FAK Apoptosis Cancer
    FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis .
    FAK-IN-2
  • HY-12289S

    VS-6063-d6; PF-04554878-d6

    FAK Isotope-Labeled Compounds Cancer
    Defactinib-d6 is a deuterium labeled Defactinib (HY-12289). Defactinib is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities .
    Defactinib-d6
  • HY-156026

    FAK Cancer
    FAK-IN-11 (Compound 4l) is a FAK inhibitor. FAK-IN-11 binds to the ATP binding pocket of FAK, and inhibits phosphorylation of FAK protein. FAK-IN-11 shows cytotoxic activity against the MDA-MB-231 cells with an IC50 of 13.73? μM. FAK-IN-11 induces non-apoptotic cell death in MDA-MB-231 cells .
    FAK-IN-11
  • HY-147520

    FAK Apoptosis Autophagy Cancer
    FAK-IN-5 (Compound 8l) is a FAK signaling inhibitor. FAK-IN-5 induces cell apoptosis and autophagy .
    FAK-IN-5
  • HY-146065

    FAK Apoptosis Cancer
    FAK-IN-4 (Compound 7d) is potential FAK inhibitor with anticancer activities. FAK-IN-4 induces cell apoptosis .
    FAK-IN-4
  • HY-150730

    FAK Cancer
    FAK-IN-6 is a potent FAK inhibitor with an IC50 value of 1.415 nM. FAK-IN-6 has anti-proliferative activity against certain cancer cell lines. FAK-IN-6 can be used for researching pancreatic cancer .
    FAK-IN-6
  • HY-145108

    FAK Cancer
    FAK-IN-1 is a FAK inhibitor with anticancer activities (WO2020231726 (Example 27)) .
    FAK-IN-1
  • HY-143458

    FAK PROTACs Cancer
    FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion .
    FAK PROTAC B5
  • HY-117836

    FAK Cancer
    FAK-IN-16 (compound OXA-11) is an orally active, selective focal adhesion kinase (FAK) inhibitor with an IC50 of 1.2 pM. FAK-IN-16 inhibits FAK phosphorylation at pFAK[Y397] and pFAK[Y861]. FAK-IN-16 slows tumor growth and reduces tumor vascularity, invasion. FAK-IN-16 potentiates effects of Cisplatin (HY-17394) on tumor cell proliferation and apoptosis in vitro and anti-tumor actions in mice .
    FAK-IN-16
  • HY-143407

    FAK Cancer
    FAK-IN-3 (Compound 36) is a potent inhibitor of focal adhesion kinase (FAK). FAK-IN-3 not only decreases migration and invasion of PA-1 cells, but also reduces expression of MMP-2 and MMP-9. FAK-IN-3 inhibits tumor growth and metastasis, and no obvious adverse effects. FAK-IN-3 has the potential for the research of ovarian cancer .
    FAK-IN-3
  • HY-156334

    FAK Cancer
    FAK-IN-12 (Compound 12S) is a FAK inhibitor (IC50 = 47 nM). FAK-IN-12 inhibits MGC-803, HCT-116 and KYSE30 cell proliferation (IC50: 0.24, 0.45, 0.44 μM). FAK-IN-12 induces apoptosis and cellular senescence .
    FAK-IN-12
  • HY-10461
    PF-573228
    15+ Cited Publications

    FAK Apoptosis Cancer
    PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for purified recombinant catalytic fragment of FAK.
    PF-573228
  • HY-149259

    FAK Cancer
    FAK-IN-9 (Compound 8f) is a potent and orally active FAK inhibitor with an IC50 of 27.44 nM. FAK-IN-9 induces triple-negative breast cancer (TNBC) cell apoptosis .
    FAK-IN-9
  • HY-148109

    FAK Cancer
    FAK-IN-7 (compound 5r) is a FAK inhibitor (IC50=11.72 µM). FAK-IN-7 has good anti-proliferative activity and can be used in cancer research .
    FAK-IN-7
  • HY-148110

    FAK Cancer
    FAK-IN-8 (compound 5h) is a FAK inhibitor (IC50=5.32 µM). FAK-IN-8 has good anti-proliferative activity and can be used in cancer research .
    FAK-IN-8
  • HY-162034

    FAK Cancer
    FAK-IN-17 is a focal adhesion kinase (FAK) inhibitor. FAK-IN-17 possesses anticancer activity against A549 and MDA-MB-231 cell lines with IC50 values of 130 nM and 94 nM .
    FAK-IN-17
  • HY-12289A
    Defactinib hydrochloride
    Maximum Cited Publications
    29 Publications Verification

    VS-6063 hydrochloride; PF 04554878 hydrochloride

    FAK Cancer
    Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.
    Defactinib hydrochloride
  • HY-160447

    Aurora Kinase FAK Cancer
    FAK/aurora kinase-IN-1 is a FAK and aurora kinase inhibitor with IC50 values of 6.61 nM and 0.91 nM, respectively. FAK/aurora kinase-IN-1 shows anticancer effects (WO2018019252A1; compound 11) .
    FAK/aurora kinase-IN-1
  • HY-153697

    FAK Cancer
    FAK-IN-10 is an inhibitor of FAK with an IC50 of 76.3 μM. FAK-IN-10 exhibits antitumor activity against MCF-7 and A431 cell lines with IC50s of 4.23 and 0.78 μM,respectively .
    FAK-IN-10
  • HY-124625

    FAK Ligands for Target Protein for PROTAC Cancer
    BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM. A PTK2 ligand for PROTAC .
    BI-4464
  • HY-132296

    FAK PROTACs Cancer
    GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect .
    GSK215
  • HY-15841

    Anaplastic lymphoma kinase (ALK) FAK Cancer
    CEP-37440 is a potent, orally active dual FAK/ALK inhibitor with IC50 values of 2.3 nM and 3.5 nM for FAK and ALK, respectively. CEP-37440 decreases the cell proliferation by blocking the autophosphorylation kinase activity of FAK1 (Tyr 397) .
    CEP-37440
  • HY-161358

    FAK Apoptosis Cancer
    FAK-IN-20 (Compound 7b) is an inhibitor of FAK with an IC50 value of 0.27 nM. FAK-IN-20 exhibits anticancer activity. It can arrest the cell cycle in the G2/M phase and induce cell apoptosis (apoptosis) by generating ROS .
    FAK-IN-20
  • HY-109084

    CT-707

    FAK Cancer
    Conteltinib (CT-707) is a multi-kinase inhibitor targeting FAK, ALK, and Pyk2. Conteltinib exerts significant inhibitory effect on FAK with an IC50 of 1.6 nM .
    Conteltinib
  • HY-155163

    Anaplastic lymphoma kinase (ALK) ROS Kinase FAK Others
    APG-2449 is an orally active ALK/ROS1/FAK inhibitor. APG-2449 shows antitumor activity in mouse models of non-small cell lung cancer (NSCLC) .
    APG-2449
  • HY-N1372A
    Fangchinoline
    4 Publications Verification

    HIV FAK Apoptosis Autophagy Infection Cancer
    Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing . Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK . Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer .
    Fangchinoline
  • HY-100498
    GSK2256098
    2 Publications Verification

    FAK Apoptosis Cancer
    GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
    GSK2256098
  • HY-157965

    VEGFR FAK Cancer
    ZINC09875266 is a dual inhibitor targeting VEGFR2 and FAK that can be used in cancer research .
    ZINC09875266
  • HY-122844

    BI-853520; IN-10018

    FAK Cancer
    Ifebemtinib (BI 853520) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1 nM). Ifebemtinib shows anti-proliferative activity against cancer cells. Ifebemtinib inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively .
    Ifebemtinib
  • HY-12289
    Defactinib
    Maximum Cited Publications
    29 Publications Verification

    VS-6063; PF-04554878

    FAK Cancer
    Defactinib (VS-6063; PF-04554878) is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities.
    Defactinib
  • HY-103471

    FAK Cancer
    Y11 inhibits FAK1 autophosphorylation by blocking phosphorylation of Y397 and decreases tumor growth .
    Y11
  • HY-B1305

    FAK Histamine Receptor VEGFR Endocrinology Cancer
    Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.
    Chloropyramine hydrochloride
  • HY-145652

    AMP-945

    FAK Cancer
    Narmafotinib (AMP-945) is an inhibitor of the enzyme focal adhesion kinase (FAK, KD=0.21 nM). Narmafotinib inhibits autophosphorylation of 397Y-FAK in MDA-MB-231 cells with an IC50=7 nM and exhibits low general cellular toxicity (IC50=2.7 μM, MDA-MB-231 cells) .
    Narmafotinib
  • HY-10458
    PF-562271 besylate
    15+ Cited Publications

    VS-6062 besylate

    FAK Pyk2 Cancer
    PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively .
    PF-562271 besylate
  • HY-122965

    FAK Akt Cancer
    Batatasin III, a stilbenoid, inhibits cancer migration and invasion by suppressing epithelial to mesenchymal transition (EMT) and FAK-AKT signals. Batatasin III has anti-cancer activities .
    Batatasin III
  • HY-W008907

    5-OTT

    Biochemical Assay Reagents Cancer
    5'-O-Tritylthymidine is an inhibitor of TK-2 and inhibits angiogenesis . 5'-O-Tritylthymidine targets FAK-Mdm-2 interactions, decreasing cell viability and increasing apoptosis.
    5'-O-Tritylthymidine
  • HY-10459
    PF-562271
    15+ Cited Publications

    VS-6062

    FAK Pyk2 Cancer
    PF-562271 (VS-6062) is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively .
    PF-562271
  • HY-N4127

    Src STAT Cancer
    3'-Demethylnobiletin, a derivative of Nobiletin, is a polymethoxyflavonoid in citrus fruits . Nobiletin exhibits anticancer activity and inhibits tumor angiogenesis by regulating Src, FAK, and STAT3 signaling .
    3'-Demethylnobiletin
  • HY-20403

    VS-6062(hydrochloride)

    FAK Pyk2 Cancer
    PF-562271 (VS-6062) hydrochloride is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively .
    PF-562271 hydrochloride
  • HY-111546

    PROTACs FAK Cancer
    BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with Cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker . Anti-cancer activity .
    BI-3663
  • HY-13917
    PND-1186
    5+ Cited Publications

    VS-4718; SR-2516

    FAK Apoptosis Cancer
    PND-1186 (VS-4718) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis .
    PND-1186
  • HY-13917A
    PND-1186 hydrochloride
    5+ Cited Publications

    VS-4718 hydrochloride; SR-2516 hydrochloride

    FAK Apoptosis Cancer
    PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis .
    PND-1186 hydrochloride
  • HY-N1127
    Tricin
    1 Publications Verification

    CMV Infection Cancer
    Tricin is a natural flavonoid found in large amounts in wheat. Tricin inhibits HCMV replication by inhibiting CDK9. Tricin inhibits the proliferation and invasion of C6 glioma cells by upregulating the expression of FAK-targeting microRNA-7 .
    Tricin

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