FAK

PF-573228 is an ATP-competitive focal adhesion kinase (FAK) inhibitor (IC 50 =4nM).

FAK Inhibitor 14 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.

Pyk2 and FAK inhibitor

focal adhesion kinase (FAK) inhibitor

TAE226(NVP-TAE226) is a potent ATP-competitive inhibitor that inhibits a variety of tyrosine protein kinases, especially FAK and IGF-IR kinases, with IC 50 values ​​of 5.5nM and 140nM, respectively.

PF-562271 (VS-6062) hydrochloride is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively.

Masitinib (AB1010) (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity.

PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively.

A potent FAK inhibitor

FAK/ALK inhibitor,potent and selective

PF-562271 is a potent small-molecule inhibitor of focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (Pyk2) with a IC 50 of 1.5 and 14nmol/L, respectively.

FAK phosphorylation inhibitor

SU6656 is a small-molecule indolinone that selectively inhibits Src, Yes, and Fyn at IC 50 values of 0.28μM, 0.02μM, and 0.17μM, respectively.

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

Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.

NAMI-A is a ruthenium-based drug characterised by the selective activity against tumour metastases, inhibits the adhesion and migration.

BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM. A PTK2 ligand for PROTAC.

Conteltinib (CT-707) is a multi-kinase inhibitor targeting FAK, ALK, and Pyk2. Conteltinib exerts significant inhibitory effect on FAK with an IC50 of 1.6 nM.

Defactinib hydrochloride is a small molecule kinase inhibitor that selectively inhibits FAK and Pyk2.

FAK inhibitor 2 is a potent focal adhesion kinase (FAK) inhibitor with an IC50 ?of 0.07?nM, with antitumor and anti-angiogenesis activities.

PROTAC FAK degrader 1 is a selective and potent von Hippel-Lindau-based focal adhesion kinase (FAK) degrader with an IC50 of 6.5 nM, DC50 of 3 nM.

An alkaloid with diverse biological activities

Petunidin is an O-methylated anthocyanidin derived from delphinidin that imparts blue-red pigments to flowers, fruits, and red wine.

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.