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FAK+inhibitor

" in MedChemExpress (MCE) Product Catalog:

47

Inhibitors & Agonists

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12289
    Defactinib
    Maximum Cited Publications
    57 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-10461
    PF-573228
    30+ 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-12444
    Y15
    25+ 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-122844
    Ifebemtinib
    3 Publications Verification

    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-12289A
    Defactinib hydrochloride
    Maximum Cited Publications
    57 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-132296
    GSK215
    2 Publications Verification

    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-144448
    FAK-IN-2
    1 Publications Verification

    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-148070

    FLT3 FAK Cytochrome P450 Cancer
    FLT3-IN-17 inhibits CYPs and FLT3 mutants activity (IC50s: <0.5 nM for D835Y). FLT3-IN-17 is also a FAK inhibitor, with an IC50 value of 12 nM. FLT3 ligand-2 can be used in the research of cancers .
    FLT3-IN-17
  • HY-122844A
    Ifebemtinib hydrochloride
    3 Publications Verification

    BI-853520 hydrochloride; IN-10018 hydrochloride

    FAK Cancer
    Ifebemtinib (BI-853520) hydrochloride is an orally active and potent focal adhesion kinase (FAK) inhibitor (IC50 = 1 nM for recombinant FAK). Ifebemtinib hydrochloride exhibits antiproliferative activity against cancer cells .
    Ifebemtinib hydrochloride
  • 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-145108

    FAK Cancer
    FAK-IN-1 is a FAK inhibitor with anticancer activities (WO2020231726 (Example 27)) .
    FAK-IN-1
  • HY-100498A
    GSK-2256098 hydrochloride
    5+ Cited Publications

    FAK Apoptosis Cancer
    GSK-2256098 hydrochloride is a focal adhesion kinase (FAK) inhibitor that exhibits potential antiangiogenic and antineoplastic activities. GSK-2256098 hydrochloride targets FAK to inhibit tumor cell growth by regulating cell adhesion, migration, proliferation, and survival.
    GSK-2256098 hydrochloride
  • HY-128580
    FAK inhibitor 2
    2 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 .
    FAK inhibitor 2
  • 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-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-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-12289R

    VS-6063 (Standard); PF-04554878 (Standard)

    FAK Reference Standards Cancer
    Defactinib (Standard) is the analytical standard of Defactinib. This product is intended for research and analytical applications. Defactinib (VS-6063; PF-04554878) is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities.
    Defactinib (Standard)
  • HY-178969

    FAK Pyk2 Apoptosis Neurological Disease Cancer
    GZD-257 is a brain-penetrant, ATP-competitive FAK inhibitor (IC50 = 14.3 nM), performing 4.77-fold selectivity with FAK to Pyk2 (IC50 = 68.2 nM). GZD-257 can significantly induce apoptosis of U118MG cells and arrest the cell cycle at the G2/M phase. GZD-257 can be used for the study of Glioblastoma (GBM) .
    GZD-257
  • HY-18928

    FAK Cancer
    FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range .
    FAK inhibitor 5
  • 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-162879

    FAK Src Akt Autophagy Cancer
    FAK inhibitor 7 is a type of FAK inhibitor with an IC50 value of 3.58 nM. FAK inhibitor 7 can inhibit the downstream signaling cascades of FAK (like Src and AKT), causing ovarian cancer cells to stall in the G0/G1 phase and induce cytotoxic autophagy. FAK inhibitor 7 can also suppress tumor metastasis and growth in ovarian cancer mice .
    FAK inhibitor 7
  • HY-116497

    FAK Cancer
    PH11 is a novel focal adhesion kinase (FAK) inhibitor that rapidly induces apoptosis in TRAIL-resistant PANC-1 cells when combined with TRAIL, but has no effect on normal human fibroblasts. The study found that PH11 downregulates c-FLIP through inhibition of FAK and phosphatidylinositol-3-kinase (PI3K)/AKT pathways, thereby restoring the TRAIL apoptotic pathway, suggesting that this combination therapy may provide an attractive therapeutic strategy for the safe and effective treatment of pancreatic cancer. PH11 selectively inhibits c-FLIP expression by modulating upstream signaling pathways and may represent an innovative therapeutic strategy. Although further work is needed to fully elucidate the mechanism of PH11-induced TRAIL sensitization, we believe that our results will provide a new approach to target c-FLIP without the risk of interfering with caspase-8 processing, which could potentially lead to TRAIL resistance. This study also suggests a role for the FAK/AKT signaling pathway in regulating c-FLIP expression in TRAIL-induced apoptosis, and this understanding will provide important clues to control the resistance mechanism to optimize the potential of TRAIL-based pancreatic cancer treatment.
    PH11
  • 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.
    FAK inhibitor 6
  • 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-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-169319

    FAK Cancer
    FAK-IN-21 (compound 9) is a FAK inhibitor with the IC50 of 37.52 nM. FAK-IN-21 inhibits cell growth and the phosphorylation of FAK. FAK-IN-21 can be used for study of diffuse gastric cancer .
    FAK-IN-21
  • HY-10461R

    Reference Standards FAK Apoptosis Cancer
    PF-573228 (Standard) is the analytical standard of PF-573228. This product is intended for research and analytical applications. PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for purified recombinant catalytic fragment of FAK.
    PF-573228 (Standard)
  • HY-12289AR

    VS-6063 hydrochloride (Standard); PF 04554878 hydrochloride (Standard)

    FAK Reference Standards Cancer
    Defactinib (hydrochloride) (Standard) is the analytical standard of Defactinib (hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • 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-173603

    FAK Cancer
    FAK-IN-27 (compound 8A) is a potent and selective FAK inhibitor with an IC50 of 4.968 nM. FAK-IN-27 suppresses H1299 cells proliferation with an IC50 of 0.28 μM. FAK-IN-27 can be used in the study of NSCLC .
    FAK-IN-27
  • 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-173495

    FAK Apoptosis Cancer
    FAK-IN-25 (4c) is a FAK inhibitor with an IC50 of 50.98 nM. FAK-IN-25 (4c) induces apoptosis and causes cell cycle arrest at G1 phase. FAK-IN-25 (4c) can be used in cancer research .
    FAK-IN-25
  • 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-170936

    FAK Hippo (MST) YAP Cancer
    MY-1576 is a FAK inhibitor with an IC50 of 8 nM. MY-1576 can activate the Hippo pathway, thereby blocking the regulation of YAP/TAZ. MY-1576 also effectively inhibits tumor growth in the KYSE30 xenograft mouse model, demonstrating good safety, and effectively downregulates the autophosphorylation of FAK and the levels of YAP/TAZ in vivo .
    MY-1576
  • 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-163715

    FAK Cancer
    Antitumor agent-165 (Compound 10l) is a potent focal adhesion kinase (FAK) inhibitor. Antitumor agent-165 exhibits effective antiproliferative activity against CAPAN-1, PANC-1, PATU-T, SUIT-2, BxPC-3, PDAC-3 and PANC-1 GR with IC50s in the range of 1.04-3.44 μM .
    Antitumor agent-165
  • HY-173515

    FAK Cancer
    FAK-IN-26 is a BBB-penetrable Focal Adhesion Kinase (FAK) inhibitor (IC50: 0.87 nM). FAK-IN-26 significantly suppresses tumor cell viability, cancer stem cell activity, and cell migration in A549 and SKOV-3 cell lines. FAK-IN-26 has potent anti-cancer activity in A549 and SKOV-3 tumor mice models with tumor inhibition rates of 59.15 % and 57.9 % .
    FAK-IN-26
  • HY-168899

    FAK Apoptosis Cancer
    FAK-IN-24 (Compound 9f) is a FAK inhibitor (IC50: 0.815 nM). FAK-IN-24 induces DNA damage and apoptosis. FAK-IN-24 has anti-glioblastoma activity. FAK-IN-24 inhibits proliferation of glioblastoma cell lines U87-MG (IC50 = 15 nM) and U251 (IC50 = 20 nM). FAK-IN-24 inhibits tumor growth in U87-MG xenograft model .
    FAK-IN-24
  • HY-175039

    FAK Apoptosis Reactive Oxygen Species (ROS) Caspase Cancer
    FAK-IN-28 is an orally active FAK inhibitor (IC50 = 0.4 nM). FAK-IN-28 exhibits dual antiproliferative and anti-metastatic properties. FAK-IN-28 triggers caspase-3-dependent apoptosis via ROS elevation. FAK-IN-28 inhibits tumor growth without causing weight loss or hepatotoxicity. FAK-IN-28 is useful in the study of FAK-driven malignancies, such as colon cancer, cervical cancer, triple-negative breast cancer, and melanoma .
    FAK-IN-28
  • HY-160411

    FAK Cancer
    FAK-IN-18 is a focal adhesion kinase (FAK) inhibitor with an IC50 of .84 nM. FAK-IN-18 can be used for the research of gastric cancer .
    FAK-IN-18
  • HY-183697

    FAK Cancer
    FAK-IN-30 is a focal adhesion kinase (FAK) inhibitor with moderate cytotoxicity against breast cancer cells. FAK-IN-30 can be used for the research of triple-negative breast cancer .
    FAK-IN-30
  • HY-183946

    FAK Cancer
    NVP-TAC544 is a focal adhesion kinase (FAK) inhibitor. NVP-TAC544 inhibits angiogenesis. NVP-TAC544 can be used for the research of melanoma (primary or metastatic) .
    NVP-TAC544
  • HY-179679

    FAK Apoptosis Cancer
    FAK-IN-29 is a selective FAK inhibitor with an IC50 of 0.5 nM. FAK-IN-29 can inhibit the proliferation and colony formation of MDA-MB-231 cells, and induce cell cycle arrest and apoptosis. FAK-IN-29 exhibits antitumor activity and can be used for the research of tumors such as triple-negative breast cancer .
    FAK-IN-29
  • HY-183769

    FAK Ligands for Target Protein for PROTAC Cancer
    FAK-IN-31 is a FAK inhibitor with antiproliferative activity against a variety of cancer cell lines. FAK-IN-31 serves as a PROTAC target protein ligand for the development of FAK-targeted PROTAC degrader heads, such as PROTAC FAK degrader 5 (HY-183768). FAK-IN-31 can be used in the research of colorectal cancer, pancreatic cancer, breast cancer, hepatocellular carcinoma and lung cancer .
    FAK-IN-31
  • HY-183284

    FAK ERK Apoptosis Neurological Disease Cancer
    GZD-552 is a potent orally active FAK inhibitor with a human FAK IC50 of 5.8 nM. GZD-552 suppresses FAK phosphorylation activation and downstream ERK signaling. GZD-552 induces apoptosis and G2/M cell cycle arrest, and exhibits antiproliferative activities in glioblastoma multiforme cells. GZD-552 exhibits antitumor efficacy in mice xenograft model. GZD-552 can be used for the research of glioblastoma multiforme .
    GZD-552
  • HY-181061

    COX EGFR Lipoxygenase FAK Raf Apoptosis Caspase Bcl-2 Family Cancer
    COX/5-LO-IN-2 is a COX2, EGFR, COX1, 5-LOX, BRAF and FAK inhibitor with IC50 of 1.22 μM, 2.5 μM, 2.95 μM, 4.65 μM, 7.4 μM, 12.2 μM, respectively. COX/5-LO-IN-2 induces cell growth arrest at G2/M phase. COX/5-LO-IN-2 triggers apoptotic activity by up-regulating proapoptotic proteins p53, Bax, and caspase-7 and down-regulating anti-apoptotic protein Bcl-2. COX/5-LO-IN-2 can be used for the research of breast cancer .
    COX/5-LO-IN-2

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