FAK

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

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

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.

OXA-11 (FAK-IN-16) is an orally active, selective focal adhesion kinase (FAK) inhibitor with antitumor activity. It inhibits FAK phosphorylation at tyrosine 397 in a dose-dependent manner and suppresses TOV21G tumor growth. It is used in cancer research.

Ifebemtinib FA (BI-853520 FA) is an orally active and potent inhibitor of adhesion patch kinase (FAK) with anticancer and antiproliferative activity for the study of ovarian and lung cancer.

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

Corosolic acid (Colosic acid) contains anti-angiogenic activity that can suppress FAK signaling induced by angiopoietin-1. Corosolic acid exerts anticancer activities against HCC, colon, and colorectal Y cells, by inducing apoptosis and promoting the N-terminal phosphorylation and subsequent proteasomal degradation of β-catenin.

PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).

NAMI-A, a ruthenium-based compound, selectively targets tumor metastasis by inhibiting cancer cell adhesion and migration.

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.

Fangchinoline (Tetrandrine B) is extracted from Stephania tetrandra S. Moore.

Y15 (1,2,4,5-Benzenetetramine tetrahydrochlor) is a potent and specificsmall-molecule FAK scaffolding inhibitor that inhibits its autophosphorylation activity, blocks tumor growth.

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

SU 6656 is a selective inhibitor of Src family kinases, with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.

PF-573228 is an ATP-competitive FAK inhibitor. In a cell-free assay, the IC50 of FAK is 4 nM.

Masitinib mesylate (AB-1010 mesylate) is a selective, orally bioavailable c-Kit inhibitor with an IC50 of 200 nM for human recombinant c-Kit, and IC50 values of 540 800 nM and 510 nM for PDGFRα β and LynB, respectively.

CEP-37440 is an effective and specific Dual FAK ALK inhibitor with IC50s of 120 nM(ALK cellular in 75% human plasma) and 2.3 nM (FAK).

AMP-945 is a proprietary focal adhesion kinase (FAK) inhibitor.

GSK2256098 (GTPL7939) is a small molecule FAK kinase inhibitor.

Chloropyramine hydrochloride (Alergosan) is a histamine receptor H1 antagonist.

BMS-536924 (BMS 536924) is an ATP-competitive IGF-1R IR inhibitor with IC50 of 100 nM 73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1 2.

1. Nitidine chloride has inhibitory effects on various tumors, such as renal cancer , breast cancer. 2. Nitidine chloride inhibits the proliferation of SMMC-7721 cells in vitro in a time- and dose-dependent manner and identifies efficacy in vivo in a mouse model of HCC.

ALK inhibitor 2 is a new-type and selective inhibitor for the ALK kinase.

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-562271 besylate (PF-00562271 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-431396 is a dual PYK2 FAK inhibitor (IC50: 11 2 nM).

Inulicin (1-O-Acetylbritannilactone), an active compound isolated from Inula Britannica L, inhibits VEGF-mediated activation of Src and FAK.

AZ7550, an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).

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.

NVP-TAE 226 (TAE226) is a potent FAK inhibitor (IC50: 5.5 nM), exhibiting even greater efficacy against Pyk2 (IC50: 3.5 nM), and is 10- to 100-fold less effective against IGF-1R, InsR, c-Met, and ALK.

(R)-Fangchinoline ((+)-Thalrugosine) is extracted from Stephania tetrandra S. Moore.

Conteltinib (CT-707) is an enzyme inhibitor with antitumor activity targeting FAK, ALK, and Pyk2.Conteltinib exhibits significant inhibition of FAK, overcomes hypoxia-mediated sorafenib resistance in hepatocellular carcinoma through inhibition of YAP signaling, and can be used in advanced ALK-positive non-small-cell lung cancer and lymphoma.

BI-4464, a highly selective ATP-competitive inhibitor of PTK2 FAK, exhibits an IC50 of 17 nM and serves as a PTK2 ligand for PROTAC (Proteolysis Targeting Chimera).

Defactinib hydrochloride (PF 04554878 hydrochloride) is a novel inhibitor of FAK. Which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.

Roslin 2 bromide (Benzylhexamethylenetetramine bromide) is a p53 reactivator that disrupts the binding of FAK and p5, exhibiting anticancer effects.

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

ALK inhibitor 1 is a selective ALK kinase inhibitor.

YH-306 (TRV055 acetate ) is a modulator of the FAK signaling pathway that acts by suppressing colorectal tumor growth and metastasis.

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

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.

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.

Compound 1T-0219 (SC) is a blocker of AKT1-FAK interaction reducing the stimulation of FAK phosphorylation in response to extracellular pressure in human SW620 colon cancer cells without affecting basal FAK phosphorylation.

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.

Compound 2119738-71-3 interacts with the FAK receptor.

ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A shows comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability.Excisanin A induces apoptosis in colon cancer cell line SW620 as determined by Annexin V staining, the cleavage of caspase-3 and the proteolytic degradation of poly (ADP-ribose) polymerase (PARP).

Defactinib analogue-1 (Compound 7) serves as a ligand for the target protein FAK, and is utilized in the synthesis of PROTAC FAK degrader 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].

Si306, an Src inhibitor, exhibits antitumor activity by reducing the phosphorylation of focal adhesion kinase (FAK) and the expression of epidermal growth factor receptor (EGFR), thereby inhibiting the invasion of human glioblastoma (GBM).