FAK

Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.

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

Ifebemtinib (BI-853520, IN-10018) is an orally active and potent inhibitor of focal adhesion kinase (FAK), with an IC50 of 1 nM against recombinant FAK. It exhibits antiproliferative activity in cancer cells and also inhibits FER and FES kinases, with IC50 values of 900 nM and 1040 nM, respectively.

AT-533 is a potent inhibitor of heat shock protein 90 (Hsp90) and herpes simplex virus (HSV), exhibiting strong antitumor and antiviral activities. It suppresses tumor growth and angiogenesis by disrupting the HIF-1α/VEGF/VEGFR-2 signaling axis, a critical pathway in tumor vascularization and progression. Additionally, AT-533 inhibits key downstream signaling cascades, including Akt/mTOR/p70S6K, ERK1/2, and FAK pathways. In endothelial cells, specifically human umbilical vein endothelial cells (HUVECs), AT-533 effectively inhibits tube formation, cell migration, and invasion, highlighting its anti-angiogenic properties. These combined effects position AT-533 as a promising candidate for cancer therapy and angiogenesis-related disease research.

Keracyanin chloride is an orally active anthocyanin compound with potent antioxidant, anti-inflammatory, and hypoglycemic properties. It exerts its biological effects by inhibiting the NF-κB/FAK/MAPK signaling pathways, which are central to inflammation, cell adhesion, and metabolic regulation.

FAK Inhibitor 7 is a potent focal adhesion kinase (FAK) inhibitor with an IC50 of 3.58 nM. This compound disrupts downstream signaling pathways associated with FAK, including Src and AKT, leading to cell cycle arrest in the G0/G1 phase and promoting cytotoxic autophagy in ovarian cancer cells. Additionally, FAK Inhibitor 7 has demonstrated efficacy in inhibiting tumor metastasis and growth in preclinical ovarian cancer mouse models, making it a valuable tool for studying cancer biology and therapeutic interventions.

FAK-IN-22 is a selective inhibitor of focal adhesion kinase (FAK) with additional activity against JAK3 and Aurora B, exhibiting IC50 values of 50.94 nM, 9.99 nM, and 0.49 nM, respectively. This compound demonstrates significant anti-tumor effects in pancreatic ductal adenocarcinoma (PDAC) by inhibiting cell proliferation, inducing apoptosis, and causing G2/M phase arrest in PANC-1 cells, with an IC50 of 0.15 μM. FAK-IN-22’s action is primarily mediated through the inhibition of the FAK/PI3K/Akt signaling pathway, making it a valuable tool for studying cancer cell dynamics and signaling mechanisms.