FAK

FAK

FAK (Focal Adhesion Kinase, or PTK2) is a protein tyrosine kinase that is not associated with receptors and is not located on membranes. It is activated at the sites of integrin clustering and cell-matrix adhesions by autophosphorylation (at Tyr397), Src, and other tyrosine kinases. By transferring signals governing cell migration, adhesion, and survival from the extracellular matrix to the cytoplasm, FAK mediates integrin-based cell signaling.

Many tumors, including those from the head and neck, colon, breast, prostate, liver, and thyroid, overexpress FAK. Additionally, in these tumors, FAK overexpression is strongly associated with an invasive phenotype. Glioblastomas and ovarian cancer cells are less likely to invade when dominant-negative FAK fragments are overexpressed and FAK signaling is inhibited. FAK is a crucial target for the creation of anti-metastatic and anti-neoplastic medications.

FAK related products

Structure Cat No. Product Name CAS No. Product Description
V69723 Adhesamine 462605-73-8 Adhesamine is a dumbbell-shaped molecule that activates the MAPK/FAK pathway.
V69722 Batatasin III 56684-87-8 Batatasin III is a stilbene compound that can inhibit cancer migration and invasion by inhibiting epithelial-mesenchymal transition (EMT) and FAK-AKT signaling.
V4437 BI-4464 1227948-02-8 BI-4464 is a novel, potent and highly selective ATP competitive inhibitor ofPTK2/FAKwith anIC50of 17 nM.
V3209 Defactinib HCl 1073160-26-5 Defactinib HCl (formerly known as VS-6063 HCl, PF-04554878 HCl) is a novel, potent, selective, and orally bioactive small molecule inhibitor of the FAK (focal adhesion kinase), it inhibits thephosphorylation of FAK at the Tyr397 site in a time- and dose-dependent manner.
V69726 FAK inhibitor 2 2354405-14-2 FAK inhibitor 2 is a potent focal adhesion kinase (FAK) inhibitor (antagonist) with IC50 of 0.07 nM and has anti-tumor and anti-angiogenic activities.
V69728 FAK inhibitor 6 2410056-27-6 Compound 26f not only optimized to effectively inhibit the enzyme (IC50= 28.2 nM), but also showed relatively little cytotoxic effect (IC50= 3.32 μM), and induced MDA-MB-231 cell apoptosis in a dose-dependent manner, effectively blocking MDA-MB-231 cells in G0/G1 phase.
V69731 FAK-IN-1 2553215-22-6 FAK-IN-1 is a FAK inhibitor (antagonist) with anti-cancer activity (WO2020231726 (Example 27)).
V69730 FAK-IN-10 491839-65-7 FAK-IN-10 is an inhibitor (blocker/antagonist) of FAK with IC50 of 76.3 μM.
V79377 FAK-IN-11 FAK-IN-11 (Compound 4l) is a FAK inhibitor.
V79378 FAK-IN-12 FAK-IN-12 (Compound 12S) is a FAK inhibitor (IC50 = 47 nM).
V69721 FAK-IN-14 2766666-22-0 FAK-IN-14 (compound 8d) is a focal adhesion kinase (FAK) inhibitor (antagonist) with IC50 of 0.2438 nM.
V79379 FAK-IN-15 FAK-IN-15 (Compound 9b) is a focal adhesion kinase (FAK) inhibitor (antagonist) with IC50 of 0.2691 nM.
V85852 FAK-IN-17
V84577 FAK-IN-19 863599-15-9
V69724 FAK-IN-2 2872588-02-6 FAK-IN-2 is a potent and orally bioactive focal adhesion kinase (FAK) inhibitor (antagonist) with anti-tumor activity (FAK IC50= 35 nM).
V69729 FAK-IN-3 2882094-29-1 FAK-IN-3 (Compound 36) is a potent inhibitor of focal adhesion kinase (FAK).
V69727 FAK-IN-9 2911655-93-9 FAK-IN-9 (Compound 8f) is a potent and orally bioactive FAK inhibitor (antagonist) with IC50 of 27.44 nM.
V69720 FC-11 2271035-37-9 FC-11 is a PROTAC FAK degrader (DC90: 1 nM).
V2836 GSK2256098 1224887-10-8 GSK2256098 is a small molecule developed by GlaxoSmithKline) as a selective FAK (Focal Adhesion Kinase) kinase inhibitor to inhibit FAK activity through targeting the phosphorylation site of FAK, tyrosine (Y) 397.
V69725 Petunidin chloride 1429-30-7 Petunidin chloride is an O-methylated anthocyanin derived from silymarin.
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