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

FAK

PTK2 protein tyrosine kinase 2; PTK2; Focal adhesion kinase

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.

FAK Related Products (51):

Cat. No. Product Name Effect Purity
  • HY-12289
    Defactinib
    Inhibitor 99.87%
    Defactinib (VS-6063; PF-04554878) is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities.
  • HY-10461
    PF-573228
    Inhibitor 99.66%
    PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for purified recombinant catalytic fragment of FAK.
  • HY-12444
    Y15
    Inhibitor 98.22%
    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.
  • HY-10209
    Masitinib
    Inhibitor 99.98%
    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.
  • HY-10459
    PF-562271
    Inhibitor 99.68%
    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.
  • HY-122844
    BI-853520
    Inhibitor 99.50%
    BI 853520 (IN-10018) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1 nM). BI 853520 shows anti-proliferative activity against cancer cells.
  • HY-148109
    FAK-IN-7
    Inhibitor 98.55%
    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.
  • HY-N10535
    Lewis y tetrasaccharide
    Activator
    Lewis Y tetrasaccharide (Lewis Y, LeY) is a tetrasaccharide derivative form of Lewis X trisaccharide (HY-N10534). Lewis Y tetrasaccharide is an antigen associated with malignant ovarian carcinomas metastasis and poor prognosis.
  • HY-13917
    PND-1186
    Inhibitor 99.80%
    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.
  • HY-B0789
    SU6656
    Inhibitor 98.05%
    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.
  • HY-100498
    GSK2256098
    Inhibitor 99.74%
    GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
  • HY-12289A
    Defactinib hydrochloride
    Inhibitor 98.95%
    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.
  • HY-13203
    NVP-TAE 226
    Inhibitor 99.92%
    NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC50s of 3.5 nM and 44 nM, respectively.
  • HY-119932
    PROTAC FAK degrader 1
    Inhibitor 99.87%
    PROTAC FAK degrader 1 is a selective and potent von Hippel-Lindau-based focal adhesion kinase (FAK) degrader with an IC50 of 6.5 nM, DC50 of 3 nM.
  • 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.
  • HY-15841
    CEP-37440
    Inhibitor 99.58%
    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).
  • HY-N0498
    Nitidine chloride
    Inhibitor 99.61%
    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. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.
  • HY-111546
    BI-3663
    Inhibitor 99.90%
    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.
  • HY-10458
    PF-562271 besylate
    Inhibitor 99.17%
    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.
  • HY-15358
    ALK inhibitor 2
    Inhibitor 99.57%
    ALK inhibitor 2 (compound 18) is a potent pyrimidin ALK inhibitor. ALK inhibitor 2 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=37 nM) and focal adhesion kinase (FAK; IC50=5 nM).