FAK

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

ALK inhibitor 1 is a selective ALK kinase inhibitor.

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

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

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

FAK-IN-1 is a FAK inhibitor with anticancer activities (WO2020231726 (Example 27)).

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.

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

PROTACFAKdegrader 3 is a selective FAK PROTAC degrader (DC50 = 1.08 nM). It induces FAK degradation through the ubiquitin-proteasome system and its interaction with FAK and CRBN. By inhibiting FAK's non-catalytic activity, PROTACFAKdegrader 3 enhances MHC-I gene transcription and tumor cell surface expression, leading to increased antigen presentation and activation of cytotoxic CD8 T cells. Its ability to promote MHC-I expression and boost T cell activation strengthens its antitumor efficacy in vivo. PROTACFAKdegrader 3 is applicable to cancer research targeting FAK degradation, including studies on ovarian cancer and hepatocellular carcinoma.

Body Protection Compound 157 (BPC 157) is a pentadecapeptide derived from BPC, identified in gastric juice, exhibiting diverse biological activities. At 2 µg/ml, BPC 157 enhances primary rat tendon fibroblast cell migration and F-actin formation. Furthermore, doses of 0.01 and 10 µg/kg, intraperitoneally (i.p.), mitigate paw swelling, bone erosion, and mononuclear cell infiltration in the joints of rats with rheumatoid arthritis induced by complete Freund's adjuvant (CFA). It also diminishes gastric ulcer size in rats caused by indomethacin, aspirin, or diclofenac at these doses. Additionally, BPC 157 reduces catalepsy duration and tremor severity in a mouse model of Parkinson's disease triggered by MPTP.

A unique collection of xnum HIF-1 related small chemicals can be used for drug discovery in ischemic disease and cancer and related mechanism studies;

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.

Adhesamine diTFA, a dumbbell-shaped molecule, activates the MAPK/FAK pathway. It promotes adhesion and growth in mammalian cells and accelerates differentiation and enhances the survival rate of primary cultured mouse hippocampal neurons.

VnP-16 enhances bone formation by stimulating the differentiation and activity of osteoblasts via direct β1 integrin engagement, which subsequently activates

FAK PROTAC B5: a degrader with 14.9 nM IC50, strong degradation, anti-growth, good plasma stability, and fair permeability.

GSK215: potent, selective PROTAC degrader of FAK (pDC50=8.4), combines FAK inhibitor VS-4718 and VHL E3 ligase binder, causes fast, lasting FAK degradation.

FAK-IN-9 (8f) is a potent oral FAK inhibitor, IC50 of 27.44 nM; induces TNBC cell apoptosis.

FAK-IN-27 (compound 8A) is a potent and selective inhibitor of FAK, with an IC50 of 4.968 nM. It effectively inhibits the proliferation of H1299 cells, with an IC50 of 0.28 μM, and is applicable for research in non-small cell lung cancer (NSCLC).

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

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