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.
All Product Categories
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FAK Related Products (193)
Related Products (193)
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Antibodies (6)
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PF-573228
0 ImagesPF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for purified recombinant catalytic fragment of FAK.
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PF-562271
0 ImagesSynonyms: VS-6062PF-562271 (VS-6062) is an orally active, ATP-competitive, reversible FAK/Pyk2 inhibitor, with an IC50 of 1.5 nM for FAK and 13 nM for Pyk2. PF-562271 induces tumor regression, and inhibits tumor growth, invasion and metastasis. PF-562271 exerts no effect on tumor necrosis, angiogenesis or apoptosis in an orthotopic mouse model of pancreatic ductal adenocarcinoma. When combined with Sunitinib (HY-10255A), PF-562271 reduces tumor vascularization, decreases serum alpha-fetoprotein levels and improves cachexia. PF-562271 can be used in research related to prostate cancer, breast cancer, pancreatic cancer, colon cancer, glioblastoma, lung cancer, pancreatic ductal adenocarcinoma and hepatocellular carcinoma.
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Ifebemtinib
0 ImagesSynonyms: BI-853520; IN-10018Ifebemtinib (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.
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Ganglioside GM2
0 ImagesGanglioside GM2 is a human tumor antigen predominantly found in human tumor cells and fetal brain tissue. As a sialylated glycosphingolipid, Ganglioside GM2 is involved in processes such as cell signaling, adhesion, and motility. Ganglioside GM2 abnormal expression and accumulation are associated with tumors and neurodegenerative disorders. Ganglioside GM2 promotes tumor cell migration and invasion by directly binding to the integrin β1 receptor, activating the FAK/Src/Erk-MAPK signaling pathway, and inducing actin cytoskeleton remodeling.
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Keracyanin chloride
0 ImagesSynonyms: Cyanidin 3-rutinoside chloride; Cyanidin 3-O-rutinoside chloride; Sambucin chlorideKeracyanin chloride inhibits NF-κB/FAK/MAPK signaling pathway. Keracyanin chloride exhibits antioxidant, anti-inflammatory and hypoglycemic effects, and is orally active.
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Creosol
0 ImagesSynonyms: 2-Methoxy-4-methylphenolCreosol (2-Methoxy-4-methylphenol) is an endogenous metabolite that acts as an important chemical intermediate and potential biofuel mainly derived from lignocellulosic biomass. Creosol is blood brain barrier penetrable.
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ZINC40099027
0 ImagesZINC40099027 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.
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Demethylzeylasteral
0 ImagesDemethylzeylasteral 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].
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Masitinib
0 ImagesSynonyms: AB1010Masitinib (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.
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GSK2256098
0 ImagesGSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
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BPC 157
0 ImagesBPC 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.
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Fangchinoline
0 ImagesFangchinoline 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.
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Nitidine chloride
0 ImagesNitidine 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.
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GSK215
0 ImagesGSK215 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.
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Defactinib hydrochloride
0 ImagesSynonyms: VS-6063 hydrochloride; PF 04554878 hydrochloride
