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.
| 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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