FAK Inhibitor

Pyk2-IN-2 (compound 13j) is an inhibitor of Pyk2 with an IC₅₀ of FAK kinase of 0.608 μM.

NAMI-A is a ruthenium-based drug characterised by the selective activity against tumour metastases, inhibits the adhesion and migration.

PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC₅₀: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 acetate exerts potent antitumor activity in tumor xenograft mouse models..

I194496 is a potent cystathionine γ-lyase (CSE) inhibitor, with an IC₅₀ of 0.79 mM. I194496 can inhibit the growth of human TNBC cells via the dual targeting PI3K/Akt and Ras/Raf/ERK pathway and suppress the metastasis of human TNBC cells via down-regulating Anxa2/STAT3 and VEGF/FAK/Paxillin signaling pathways.

T7 Peptide TFA is a protein synthesis inhibitor and anti-angiogenic agent, with a K_d of 10 nM for human transferrin receptor. T7 Peptide TFA inhibits the phosphorylation of focal adhesion kinase, the activation of phosphatidylinositol 3-kinase and Akt, the kinase activity of mTOR, as well as the phosphorylation of 4E-BP1 in endothelial cells. T7 Peptide TFA induces G0/G1 cell cycle arrest, apoptosis and protective autophagy in hepatocellular carcinoma cells, and suppresses tumor growth in mouse models. T7 Peptide TFA is applicable to research related to cancer, glioblastoma, hepatocellular carcinoma and glioma.

ALK inhibitor 2 (compound 18) is a potent pyrimidin ALK inhibitor. ALK inhibitor 2 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC₅₀=37 nM) and focal adhesion kinase (FAK; IC₅₀=5 nM).

Pongamol (Lanceolatin C) is an orally active flavonoid with an IC₅₀ of 75 μM and a K_i of 58 μM against PTPase-1B, and an IC₅₀ of 103.5 μM against intestinal α-Glycosidase. Pongamol reduces the release of IL‑1β, TNF‑α, COX‑2 and iNOS in cells, reverses the nuclear translocation of NF‑κB, and upregulates the levels of Beclin 1 and LC3 Ⅱ/LC3 Ⅰ. Pongamol promotes glucose uptake by increasing the level of GLUT4 on the surface of skeletal muscle cells. Pongamol inhibits epithelial-mesenchymal transition by suppressing the FAK/Akt-mTOR signaling pathway. Pongamol inhibits neuronal cytotoxicity, suppresses cell apoptosis and extends the lifespan of Caenorhabditis elegans by activating the MAPKs/Nrf2 signaling pathway. Pongamol exerts hypoglycemic effects in diabetic mouse models. Pongamol exhibits antibacterial activity. Pongamol alleviates oxidative stress, neuroinflammation, Aβ deposition and excessive phosphorylation of Tau Protein, and restores autophagy function in Alzheimer's disease mouse models by inhibiting the Akt/mTOR signaling pathway. Pongamol is applicable to research related to Alzheimer's disease, type 2 diabetes, non-small cell lung cancer and postprandial hyperglycemia.

Conteltinib tetrahydrochloride (CT-707 tetrahydrochloride) is the tetrahydrochloride salt form of Conteltinib (HY-109084). Conteltinib tetrahydrochloride is the inhibitor for FAK (IC₅₀=1.6 nM), ALK, and Pyk2. Conteltinib tetrahydrochloride exhibits a synergistic anti-tumor efficacy with Cabozantinib (HY-13016).

FAK-IN-19 (ligand3) is an inhibitor in a co-crystal structure with FAK. FAK-IN-19 has anticancer effects.

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

TG53 is a potent inhibitor of tissue transglutaminase (TG2) and fibronectin (FN) protein-protein interaction. TG53 inhibits formation of a complex with integrin β1 and activation of FAK and c-Src during SKOV3 cell attachment onto FN. TG53 can be used for ovarian cancer research.

MY-1576 is a FAK inhibitor with an IC₅₀ of 8 nM. MY-1576 can activate the Hippo pathway, thereby blocking the regulation of YAP/TAZ. MY-1576 also effectively inhibits tumor growth in the KYSE30 xenograft mouse model, demonstrating good safety, and effectively downregulates the autophosphorylation of FAK and the levels of YAP/TAZ in vivo.

NBM-T-BMX-OS01 (BMX) is a derivative of Osthole (HY-N0054). NBM-T-BMX-OS01 attenuates the phosphorylation levels of ERK and Akt in an AMPK-dependent manner. NBM-T-BMX-OS01 induces oxidative stress through the production of ROS. NBM-T-BMX-OS01 enhances Cisplatin-induced cell proliferation inhibition, colony formation inhibition, apoptosis (apoptosis) and cell cycle arrest. NBM-T-BMX-OS01 inhibits VEGF-induced phosphorylation of VEGFR2 and FAK. NBM-T-BMX-OS01 inhibits VEGF-induced endothelial cell proliferation, migration and tube formation, as well as microvessel sprouting in rat aortic rings and angiogenesis induced by colorectal cancer cells. NBM-T-BMX-OS01 inhibits the growth of subcutaneous colorectal cancer xenografts in nude mice. NBM-T-BMX-OS01 can be used in studies related to lung cancer, colorectal cancer and angiogenesis.

Ifebemtinib (BI-853520) hydrochloride is an orally active and potent focal adhesion kinase (FAK) inhibitor (IC₅₀ = 1 nM for recombinant FAK). Ifebemtinib hydrochloride exhibits antiproliferative activity against cancer cells.

FAK-IN-7 (compound 5r) is a FAK inhibitor (IC₅₀=11.72 µM). FAK-IN-7 has good anti-proliferative activity and can be used in cancer research.

Demethylzeylasteral (Standard) is the analytical standard of Demethylzeylasteral. This product is intended for research and analytical applications. Demethylzeylasteral is an orally active triterpenoid compound isolated from Tripterygium wilfordii, which has functions such as anti-inflammatory, anti-tumor, anti fertility, estrogen metabolism regulation, immune suppression, and immune system regulation .

IL13Rα2 D1 is an effective IL-13/IL13Rα2 signaling axis inhibitor. IL13Rα2 D1 can inhibit IL-13-induced cell adhesion, migration, invasion, and proliferation. IL13Rα2 D1 can inhibit FAK, Src, AKT, ERK1/2 phosphorylation, and MMP expression. IL13Rα2 D1 can be used for research on cancers such as colorectal cancer.

PST3.1a is an orally active and brain-penetrant N-acetylglucosamine glycosyltransferase (MGAT5) inhibitor with a human IC₅₀ of 2 µM. PST3.1a inhibits TGFβR and FAK signaling pathway activity. PST3.1a alters β1,6-GlcNAc N-glycans and microtubule/microfilament integrity, increases OLIG2 expression, and inhibits proliferation, migration, invasiveness, and clonogenic capacities of glioblastoma initiating cells. PST3.1a reduces invasive and proliferative capacity of glioblastoma initiating cells in orthotopic graft models, increases overall survival of orthotopic graft model mice. PST3.1a blunts MGAT5 overexpression, decreases renal fibrosis via collagen 1, collagen 4, and galectin 3 downregulation in a rat chronic kidney disease model. PST3.1a can be used for the research of glioblastoma multiforme and chronic kidney disease.

ULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC₅₀ of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy, and can be used to study NSCLC (Non-small cell lung cancer).

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