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 |
|---|---|---|---|---|
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V3389 | Y15 | 4506-66-5 | Y15 (also known as FAK inhibitor Y15 and FAK Inhibitor 14) is a novel, potent, specific and direct inhibitor of focal adhesion kinase (FAK) which blocks phosphorylation of Y397 with an IC50 value of about 1 μM. |
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V128262 | Active focal adhesion kinase, Human | Active focal adhesion kinase, human, is a cytosolic protein tyrosine kinase that is concentrated in adhesion focals formed between cells growing in the presence of extracellular matrix components. | |
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V69723 | Adhesamine | 462605-73-8 | Adhesamine is a dumbbell-shaped molecule that activates the MAPK/FAK pathway. |
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V96767 | Adhesamine diTFA | 1201698-09-0 | Adhesamine diTFA is a dumbbell-shaped molecule that activates the MAPK/FAK pathway. |
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V88027 | Antitumor agent-165 | Antitumor agent-165 (Compound 10l) is a potent inhibitor of focal adhesion kinase (FAK). | |
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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. |
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V115031 | BI-0319 | 2341740-85-8 | BI-0319 is a selective PTK2/FAK PROTAC degrader. |
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V4437 | BI-4464 | 1227948-02-8 | BI-4464 is a novel, potent and highly selective ATP competitive inhibitor ofPTK2/FAKwith anIC50of 17 nM. |
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V112492 | BSJ-04-146 | 2414478-45-6 | BSJ-04-146 is a highly potent and selective PROTAC-targeting focal adhesion kinase (FAK) inhibitor (IC50 = 26 nM). |
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V102536 | Conteltinib tetrahydrochloride | Continib tetrahydrochloride (CT-707 tetrahydrochloride) is the tetrahydrochloride form of continib. | |
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V118961 | FAK aa411-686 Recombinant Human Active Protein Kinase | Focal adhesion kinase (FAK) is a cytoplasmic non-receptor tyrosine kinase that can bind to integrins and growth factor receptors to regulate cell adhesion, proliferation, migration, invasion and metastasis. | |
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V135536 | FAK activator-1 | 2769848-56-6 | FAK activator-1 is a FAK activator and mucosal healing inducer. |
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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. |
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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. |
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V112018 | FAK ligand-2 | 2414478-49-0 | FAK ligand-2 is a FAK inhibitor and a ligand for the target protein of PROTAC (FAK). |
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V117008 | FAK ligand-5 | 1227948-58-4 | FAK ligand-5 is a FAK ligand. |
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V69731 | FAK-IN-1 | 2553215-22-6 | FAK-IN-1 is a FAK inhibitor (antagonist) with anti-cancer activity (WO2020231726 (Example 27)). |
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V69730 | FAK-IN-10 | 491839-65-7 | FAK-IN-10 is an inhibitor (blocker/antagonist) of FAK with IC50 of 76.3 μM. |
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V79377 | FAK-IN-11 | FAK-IN-11 (Compound 4l) is a FAK inhibitor. | |
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V79378 | FAK-IN-12 | FAK-IN-12 (Compound 12S) is a FAK inhibitor (IC50 = 47 nM). |