Signaling Pathway

FAK

FAK

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FAK (Focal Adhesion Kinase or PTK2) is a focal adhesion-associated protein kinase involved in cellular adhesion and spreading processes. It has been shown that when FAK was blocked, breast cancer cells became less metastatic due to decreased mobility. FAK is found concentrated in the focal adhesions that form among cells attaching to extracellular matrix constituents. FAK is a member of the FAK subfamily of protein tyrosine kinases that included PYK2 but lacks significant sequence similarity to kinases from other subfamilies. With the exception of certain types of blood cells, most cells express FAK. FAK tyrosine kinase activity can be activated, which plays a key important early step in cell migration. FAK activity elicits intracellular signal transduction pathways that promote the turn-over of cell contacts with the extracellular matrix, promoting cell migration.

FAK Inhibitors & Modulators (10)

Product Name Catalog No. Brief Description
Defactinib

HY-12289

Defactinib(VS-6063; PF-04554878) is a potent FAK phosphorylation inhibitor; overcomes YB-1–mediated paclitaxel
resistance by an AKT-dependent pathway.

Defactinib hydrochloride

HY-12289A

Defactinib Hcl (VS-6063; PF-04554878) is a potent FAK phosphorylation inhibitor; overcomes YB-1–mediated paclitaxel
resistance by an AKT-dependent pathway.

GSK2256098

HY-100498

GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.

NVP-TAE 226

HY-13203

NVP-TAE226 is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2(IC50=3.5 nM); 10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met.

PF-431396

HY-10460

PF-431396 is dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively), PF-431396 has a Kd value of 445 nM for BRD4.

PF-562271

HY-10459

PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.

PF-562271 besylate

HY-10458

PF-562271 besylate is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.

PF-573228

HY-10461

PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for inhibiton of purified recombinant catalytic fragment of FAK; inhibits FAK phosphorylation on Tyr(397) with an IC(50) of 30-100 nM.

PND-1186

HY-13917

PND-1186 is a potent FAK inhibitor with IC50 of 1.5 nM.

Y15

HY-12444

Y15 is a novel small molecule FAK phosphorylation inhibitor; specifically block phosphorylation of Y397-FAK and total phosphorylation of FAK.