FAK

ZINC40099027 is a specific adhesion plaque kinase (FAK) activator that promotes gastric mucosal repair in persistent aspirin-associated gastric injury through activation of adhesion plaque kinase, activates human adhesion plaque kinase by accelerating the enzyme activity of the structural domain of FAK kinase, activates cytosolic FAK, and promotes intestinal epithelial wound closure.

FAK-IN-7 has potential antiproliferative activity and is a FAK inhibitor.

FAK-IN-10 is an inhibitor of FAK (IC50: 76.3 μM) and demonstrates antitumor activity in MCF-7 and A431 cell lines with IC50 values of 4.23 μM and 0.78 μM, respectively.

PND-1186 (VS-4718) is a specific and reversible FAK inhibitor with an IC50 of 1.5 nM.

Defactinib (VS-6063) is a second-generation inhibitor of FAK that inhibits FAK phosphorylation at the Tyr397 site. Defactinib has potential antitumor activity.

Ifebemtinib (BI-853520) is an orally active and potent inhibitor of adhesion plaque kinase (FAK) (IC50=1 nM) with anti-tumour activity that inhibits globule formation and in situ tumour growth in malignant pleural mesotheliomas, and may be useful for the study of breast and ovarian cancer.

FAK inhibitor7, a potent FAK inhibitor, demonstrates an IC50 of 3.58 nM. This compound effectively inhibits downstream signaling cascades of FAK (such as Src and AKT), which leads to cell cycle arrest at the G0 G1 phase and induces cytotoxic autophagy in ovarian cancer cells. Additionally, FAK inhibitor7 has been shown to suppress tumor metastasis and growth in ovarian cancer mouse models.

FAK-IN-21 (compound 9) is a FAK inhibitor with an IC50 value of 37.52 nM. It inhibits cell growth and the phosphorylation of FAK, making it useful for research into diffuse gastric cancer.

FAK-IN-23 (Compound II) is an inhibitor of focal adhesion kinase (FAK).

FAK-IN-24 (Compound 9f) is a potent FAK inhibitor with an IC50 of 0.815 nM. It induces DNA damage and apoptosis, and exhibits activity against glioblastoma. FAK-IN-24 effectively inhibits proliferation of glioblastoma cell lines U87-MG (IC50= 15 nM) and U251 (IC50= 20 nM), and suppresses tumor growth in U87-MG xenograft models.

Masitinib (AB1010) is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet and has been available for veterinaries since 2011.

PF-03814735 is a novel, potent and reversible inhibitor of Aurora A B with IC50of 0.8 nM 5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.

FAK-IN-11 (Compound 4l), a FAK inhibitor, specifically targets the ATP binding pocket of FAK to prevent its phosphorylation. It exhibits cytotoxic effects on MDA-MB-231 cells, achieving an IC50 value of 13.73 μM, and induces non-apoptotic cell death in these cells [1].

FAK-IN-12 (Compound 12S) is a selective FAK inhibitor with an IC50 of 47 nM, effectively suppressing proliferation of MGC-803, HCT-116, and KYSE30 cells with IC50 values of 0.24, 0.45, and 0.44 μM, respectively. Additionally, FAK-IN-12 promotes apoptosis and cellular senescence [1].

Batatasin III inhibits cancer migration and invasion by suppressing epithelial to mesenchymal transition and FAK-AKT signals and possesses anti-cancer activities. Batatasin III has a long-term inhibitory effect on whole-plant growth and shows germination

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

GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader (pDC50= 8.4), designed using the FAK inhibitor VS-4718 and a binder for the VHL E3 ligase, capable of inducing rapid and prolonged FAK degradation.

FAK-IN-14 is a highly effective focal adhesion kinase (FAK) inhibitor that induces apoptosis and cell cycle arrest. FAK-IN-14 has weak inhibitory effects on Akt, c-kit, MEK1 2 and mTOR, but has significant inhibitory effects on FAK, FGFR1 and Pyk2.

FAK-IN-15 is a highly potent focal adhesion kinase (FAK) inhibitor with antitumor activity.

Mps1-IN-1 is a potent, selective, and ATP-competitive inhibitor of Mps1 kinase (IC50: 367 nM).

AZ7550 trimesylate salt (AZ7550 Mesylate) is the active metabolite of ositinib, AZ7550 trimesylate salt inhibits IGF1R activity and can be used in the study of non-small cell lung cancer.

FAK inhibitor 5 is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range.

PROTAC FAK degrader 1 is a selective and potent degrader of focal adhesion kinase (Fak) with an IC50 of 6.5 nM.

FAK ligand-Linker Conjugate 1 is a chemical compound designed to facilitate PROTAC-mediated protein degradation. This compound consists of a ligand specifically targeting FAK and a PROTAC linker module, which acts as a recruitment agent for E3 ligases including VHL, CRBN, MDM2, and IAP[1].