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.

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

Lewis Y tetrasaccharide, a derivative of Lewis X, is an antigen linked to ovarian cancer metastasis and bad prognosis.

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.

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

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

<p>Compound 2119738-71-3 interacts with the FAK receptor.</p>

<p>A unique collection of 1016 tyrosine kinase inhibitors for high throughput screening and high content screening for drug discovery in tyrosine kinase related</p>

MY-1576 is a FAK inhibitor with an IC50 of 8 nM. It activates the Hippo pathway, thereby inhibiting YAP/TAZ regulation. Additionally, MY-1576 effectively suppresses tumor growth in the KYSE30 xenograft mouse model, demonstrates good safety, and efficiently downregulates FAK autophosphorylation and YAP/TAZ levels in vivo.

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

<p>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.</p>

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.

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

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).

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.

<p>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.</p>