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.
Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
H9068 |
BJG-03-025 |
2553213-90-2 | BJG-03-025 is a potent and highly selective focal adhesion kinase (FAK) inhibitor with IC50 value of 20 nM. |
H8998 |
PND-1186 |
1061353-68-1 | PND-1186(VS-4718)is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis. |
H8997 |
PND-1186 hydrochloride |
1356154-94-3 | PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis. |
H8647 |
PF-719 |
1404454-02-9 |
PF-719 (PF719) is a potent, selective Pyk2 inhibitor with IC50 of 17 nM, displays 25-fold selectvity over FAK (IC50=469 nM); does not have significant inhibitory effects on recombinant MLCK2, p38, Akt1, or ROCK1, and very little inhibtion at Src family kinases (IC50>5 uM); selectively inhibits tyrosine phosphorylation of Pyk2 at 1 uM, but blocks both Pyk2 and FAK phosphorylation at 2.5 uM in A20 cells; reduces chemoattractant-induced migration of B-2 and MZ B cells. |
H7928 |
Y15 |
4506-66-5 | FAK inhibitor Y15 is a small molecule inhibitor targeting the main autophosphorylation site of FAK, specifically blocks phosphorylation of Y397-FAK (IC50=1 uM) and total phosphorylation of FAK; does not significantly decrease kinase activity of the other kinases (Pyk2 autophosphorylation); directly and specifically decreases Y397-phosphorylation of FAK in vitro, inhibits cancer cell viability in vitro, causes detachment, decreases cell adhesion and blocks tumor growth in vivo. |
H7927 |
TAS-301 |
193620-69-8 | An inhibitor of smooth muscle cell migration and proliferation; inhibits PDGF-induced tyrosine phosphorylation of both FAK and paxillin; also inhibits PDGF-induced elevation of [Ca2+]i and activation of CaMK II, reduces the extent of F-actin stress fiber depolymerization observed in response to PDGF at 10 uM. |
H7926 |
Pyk2-IN-25a |
2052970-45-1 | Pyk2-IN-25a is a highly potent Pyk2 (PTK2B) inhibitor with IC50 of 0.67 nM, dispalys 2-fold weakening potency for FAK (IC50=1.26 nM); a suitable tool compound for future proof-of-concept studies. |
H7925 |
PF-719 dihydrochloride |
PF-719 (PF719) is a potent, selective Pyk2 inhibitor with IC50 of 17 nM, displays 25-fold selectvity over FAK (IC50=469 nM); does not have significant inhibitory effects on recombinant MLCK2, p38, Akt1, or ROCK1, and very little inhibtion at Src family kinases (IC50>5 uM); selectively inhibits tyrosine phosphorylation of Pyk2 at 1 uM, but blocks both Pyk2 and FAK phosphorylation at 2.5 uM in A20 cells; reduces chemoattractant-induced migration of B-2 and MZ B cells. |
|
H7924 |
PF-573228 |
869288-64-2 | A potent, selective, ATP-competitive FAK inhibitor with IC50 of 4 nM; displays 250-fold selectivity over Pyk2, 50–250-fold over a panel of kinases (CDK1, CDK7, GSK3β); inhibits FAK phosphorylation on Tyr397 in cultured cells (IC50=30-100 nM), inhibits both chemotactic and haptotactic migration. |
H7923 |
PF-562271 besylate |
939791-38-5 | A potent, selective, ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase with IC50 of 1.5 nM and 14 nM, respectively; displayes robust inhibition in an inducible cell-based assay measuring phospho-FAK with IC50 of 5 nM; inhibits FAK phosphorylation in vivo in a dose-dependent fashion (EC50=93 ng/mL) after in tumor-bearing mice; orally bioavailable. |
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