fak in 1

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

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/aurora kinase-IN-1, a dual inhibitor of FAK and aurora kinase, has IC50 values of 6.61 nM and 0.91 nM respectively, and demonstrates anticancer effects (WO2018019252A1; compound 11) [1].

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].

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.

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].

FAK-IN-19 (ligand3), an inhibitor co-crystallized with FAK, exhibits anticancer effects [1].

FAK-IN-17 is an inhibitor of focal adhesion kinase (FAK). It exhibits anticancer properties with IC50 values of 130 nM in A549 cells and 94 nM in MDA-MB-231 cells.

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.

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

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

1-(2-([(2-Methylbenzoyl)oxy]imino)cyclohexyl)-2,4-dinitrobenzene is a blocker of AKT1-FAK interactions and reduces stimulation of FAK phosphorylation by extracellular stress in human SW620 colon cancer cells without affecting basal FAK phosphorylation.

Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) is a PROTAC linker characterized by its PEG composition, crucial in synthesizing various PROTACs, including BI-3663, a selective PTK2/FAK PROTAC. Using cereblon ligands, it targets E3 ligases to degrade PTK2, exhibiting potent inhibitory activity with an IC50 of 18 nM[1].

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-22 (Compound 26) is an inhibitor of FAK, JAK3, and Aurora B, with IC50 values of 50.94 nM, 9.99 nM, and 0.49 nM, respectively, effectively suppressing tumorigenesis and metastasis in pancreatic ductal adenocarcinoma (PDAC). It inhibits proliferation in PANC-1 cells with an IC50 of 0.15 μM. FAK-IN-22 induces apoptosis and G2/M phase arrest in PANC-1 cells by inhibiting the FAK/PI3K/Akt signaling pathway.

MLK3-IN-1 (Compound 37) is a selective inhibitor of mixed-lineage kinase 3 (MLK3) with an IC50 of less than 1 nM. It also inhibits FAK with an IC50 of 15.5 μM. In both murine and human liver microsomes, MLK3-IN-1 demonstrates excellent metabolic stability.

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.

FAK-IN-4 (Compound 7d) exhibits anticancer activities by inducing cell apoptosis and is a potential inhibitor of FAK [1].

FAK-IN-8 (compound 5h), a FAK inhibitor with an IC50 of 5.32 μM, exhibits potent anti-proliferative activity, making it suitable for use in cancer research [1].

FAK-IN-3 is a potent inhibitor of adherens spot kinase (FAK). FAK-IN-3 reduces migration and invasion of PA-1 cells and inhibits the expression of MMP-2 and MMP-9. FAK-IN-3 inhibits tumor growth and metastasis with no significant adverse effects. FAK-IN-3 has shown investigational potential in ovarian cancer.