2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. FAK

FAK

PTK2 protein tyrosine kinase 2; PTK2; Focal adhesion kinase

FAK

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FAK (Focal Adhesion Kinase or PTK2) is a non-receptor and non-membrane associated protein tyrosine kinase that is activated at the sites of cell-matrix adhesions and integrin clustering by auto-phosphorylation (at Tyr397), Src, and other tyrosine kinases. FAK mediates integrin-based cell signaling by transferring signals regulating cell migration, adhesion, and survival from the extracellular matrix to the cytoplasm.

FAK is overexpressed in many tumors, including those derived from the head and neck, colon, breast, prostate, liver, and thyroid. Furthermore, FAK overexpression is highly correlated with an invasive phenotype in these tumors. Inhibition of FAK signaling by overexpression of dominant-negative fragments of FAK reduces invasion of glioblastomas and ovarian cancer cells. FAK therefore represents an important target for the development of anti-neoplastic and anti-metastatic drugs.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12289
    Defactinib
    		Inhibitor 99.74%
    Defactinib (VS-6063; PF-04554878) is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities.
    Defactinib
  • HY-10461
    PF-573228
    		Inhibitor 99.32%
    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
    		Inhibitor 98.0%
    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-10459
    PF-562271
    		Inhibitor 99.36%
    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-122844
    Ifebemtinib
    		Inhibitor 99.86%
    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-P11474
    FZ1 peptide
    		Activator 99.92%
    FZ1 peptide is an integrin αvβ3 agonist. FZ1 peptide binds to integrin αvβ3, effectively activates FAK, FAK-dependent AKT and ERK1/2 signaling pathways. FZ1 peptide enhances VEGFC-induced endothelial angiogenesis, accelerates diabetic skin wound healing.
    FZ1 peptide
  • HY-151010
    FAK ligand-2
    		Inhibitor
    FAK ligand-2 is a FAK ligand and a ligand for the target protein of PROTAC (FAK). FAK ligand-2 can be used to synthesize BSJ-04-146 (HY-179512).
    FAK ligand-2
  • HY-W783415
    STARD3-IN-1
    		Activator
    STARD3-IN-1 (Compound VS1) is a STARD3 inhibitor with an IC₅₀ of 35 μM. STARD3 is a protein that is overexpressed in various cancers and is involved in cholesterol transport. STARD3-IN-1 exhibits anti-proliferative activity in breast cancer and colon cancer cells, significantly weakening the clonogenic ability of cancer cells. STARD3-IN-1 increases the protein levels of FAK and pTyr397-FAK. STARD3-IN-1 can be used for research on breast cancer and colon cancer.
    STARD3-IN-1
  • HY-134570
    ZINC40099027
    		Activator 99.97%
    ZINC40099027 is a selective FAK activator. ZINC40099027 promotes FAK phosphorylation, without activating its paralogs Pyk2 and Src. ZINC40099027 promotes the wound closure of human intestinal epithelial monolayers and the healing of mouse ulcers by activating FAK. ZINC40099027 can be used for diseases related to gastrointestinal mucosal injury research.
    ZINC40099027
  • HY-13917
    PND-1186
    		Inhibitor 99.88%
    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-B0789
    SU6656
    		Inhibitor 99.01%
    SU6656 is a Src family kinases inhibitor with IC50s of 280, 20, 130, 170 nM for Src, Yes, Lyn, and Fyn, respectively. SU6656 inhibits FAK phosphorylation at Y576/577, Y925, Y861 sites. SU6656 also inhibits p-AKT.
    SU6656
  • HY-N0587
    Demethylzeylasteral
    		Inhibitor 99.92%
    Demethylzeylasteral is an orally active triterpenoid compound isolated from Tripterygium wilfordii, which has functions such as anti-inflammatory, anti-tumor, anti fertility, estrogen metabolism regulation, immune suppression, and immune system regulation [1][2].
    Demethylzeylasteral
  • HY-10209
    Masitinib
    		Inhibitor 99.94%
    Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity.
    Masitinib
  • HY-100498
    GSK2256098
    		Inhibitor 99.86%
    GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
    GSK2256098
  • HY-N0498
    Nitidine chloride
    		Inhibitor 99.82%
    Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway, also has anti-inflammatory activity. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.
    Nitidine chloride
  • HY-N1372A
    Fangchinoline
    		Inhibitor 99.92%
    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-105174
    BPC 157
    		Activator 99.78%
    BPC 157 is the 15-amino acide fragment of gastric peptide BPC. BPC 157 exhibits wound healing promoting and neuroprotective activity. BPC 157 maintains the integrity of the gastrointestinal mucosa without significant toxicity. BPC 157 acetate counteracts NSAIDs/insulin overdose/copper-induced toxicity. BPC 157 ameliorates specific (over)stimulated/damaged neurotransmitter systems-induced behavioral disorders through serotonergic and dopaminergic systems.
    BPC 157
  • HY-132296
    GSK215
    		Inhibitor 99.26%
    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-12289A
    Defactinib hydrochloride
    		Inhibitor 99.35%
    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-10460
    PF-431396
    		Inhibitor 99.74%
    PF-431396 is an orally active dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with IC50 values of 2 nM and 11 nM, respectively.
    PF-431396
Cat. No. Product Name / Synonyms Application Reactivity