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

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-IN-1, a FAK inhibitor with anticancer activities (WO2020231726 [Example 27]).

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.

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].

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.

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

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

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.

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

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.

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

ALK inhibitor 1 is a selective ALK kinase inhibitor.

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

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.

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

BI-3663 is a highly selective PTK2/FAK PROTAC that utilizes cereblon ligands to hijack E3 ligases for PTK2 degradation, with an IC50 of 18 nM. It is composed of BI-4464 linked to Pomalidomide with a linker[1]. Anti-cancer.

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.

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.