FAK Inhibitor

FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC₅₀ values in the low micromolar range.

NEO212 is an orally active, blood-brain barrier permeable conjugate of Temozolomide (TMZ) (HY-17364) and Perillyl Alcohol (POH) (HY-N7000), with potent anticancer activity. NEO212 overcomes classical TMZ resistance and DNA alkylation by depleting MGMT. By inhibiting the FAK/Src signaling pathway, NEO212 reduces the production of MMP2 and MMP9, induces mesenchymal-epithelial transition, and inhibits the migration, invasion and tumor progression of glioma stem cells. NEO212 disrupts autophagy flux to enhance mitochondrial apoptosis; it induces differentiation of acute myeloid leukemia (AML) cells into macrophages and proliferation arrest.

Cafestol (Standard) is the analytical standard of Cafestol. This product is intended for research and analytical applications. Cafestol is an orally active diterpenoid and an inhibitor of ERK2. Cafestol has elevated blood lipids, anti-inflammatory, anti-angiogenic and anti-diabetic activities. In addition, Cafestol induces tumor cell apoptosis and autophagy, which can be used in the study of cancer.

FAK-IN-16 (compound OXA-11) is an orally active, selective focal adhesion kinase (FAK) inhibitor with an IC₅₀ of 1.2 pM. FAK-IN-16 inhibits FAK phosphorylation at pFAK[Y397] and pFAK[Y861]. FAK-IN-16 slows tumor growth and reduces tumor vascularity, invasion. FAK-IN-16 potentiates effects of Cisplatin (HY-17394) on tumor cell proliferation and apoptosis in vitro and anti-tumor actions in mice.

T7 Peptide is a protein synthesis inhibitor and anti-angiogenic agent, with a K_d of 10 nM for human transferrin receptor. T7 Peptide 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 induces G0/G1 cell cycle arrest, apoptosis and protective autophagy in hepatocellular carcinoma cells, and suppresses tumor growth in mouse models. T7 Peptide is applicable to research related to cancer, glioblastoma, hepatocellular carcinoma and glioma.

FAK-IN-8 (compound 5h) is a FAK inhibitor (IC₅₀=5.32 µM). FAK-IN-8 has good anti-proliferative activity and can be used in cancer research.

PF-562271 besylate (Standard) is the analytical standard of PF-562271 besylate (HY-10458). This product is intended for research and analytical applications. PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC₅₀ of 1.5 nM and 13 nM, respectively.

Ovalitenone is a flavonoid compound that can be isolated from the plant Millettia peguensis. It shows no cytotoxic effects on lung cancer H460 and A549 cells, but it significantly inhibits anchorage-independent growth, CSC-like phenotypes, colony formation, and the migration and invasion capabilities of cancer cells. Ovalitenone can significantly reduce the levels of N-cadherin, snail, and slug, while increasing E-cadherin, thus inhibiting the EMT pathway. Additionally, Ovalitenone suppresses the signaling pathways regulated by focal adhesion kinase (FAK), ATP-dependent tyrosine kinase (AKT), mammalian target of rapamycin (mTOR), and cell division cycle 42 (Cdc42).

NVP-TAE 226 (Standard) is the analytical standard of NVP-TAE 226. This product is intended for research and analytical applications. NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC50s of 3.5 nM and 44 nM, respectively.

GSK2256098 (Standard) is the analytical standard of GSK2256098 (HY-100498). This product is intended for research and analytical applications. GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.

PF-431396 (Standard) is the analytical standard of PF-431396 (HY-10460). This product is intended for research and analytical applications. PF-431396 is an orally active dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with IC₅₀ values of 2 nM and 11 nM, respectively.

FAK/Aurora kinase-IN-1 is a FAK and aurora kinase inhibitor with IC₅₀ values of 6.61 nM and 0.91 nM, respectively. FAK/Aurora kinase-IN-1 shows anticancer effects (WO2018019252A1; compound 11).

Protein kinase inhibitor 10 is a protein kinase inhibitor with IC₅₀ values of 28.9, 13.6, and 2.41 μM for TAM receptor, FAK, and KIT, respectively. Protein kinase inhibitor 10 can inhibit abnormal and excessive cell proliferation, showing promise for research in cancer therapy.

BI-3663 (Standard) is the analytical standard of BI-3663 (HY-111546). This product is intended for research and analytical applications. BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with Cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC₅₀ of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker. Anti-cancer activity.

PF-562271 (Standard) (VS-6062 (Standard)) is the analytical standard of PF-562271 (HY-10459). This product is intended for research and analytical applications. PF-562271 (VS-6062) is an orally active, ATP-competitive, reversible FAK/Pyk2 inhibitor, with an IC₅₀ of 1.5 nM for FAK and 13 nM for Pyk2. PF-562271 induces tumor regression, and inhibits tumor growth, invasion and metastasis. PF-562271 exerts no effect on tumor necrosis, angiogenesis or apoptosis in an orthotopic mouse model of pancreatic ductal adenocarcinoma. When combined with Sunitinib (HY-10255A), PF-562271 reduces tumor vascularization, decreases serum alpha-fetoprotein levels and improves cachexia. PF-562271 can be used in research related to prostate cancer, breast cancer, pancreatic cancer, colon cancer, glioblastoma, lung cancer, pancreatic ductal adenocarcinoma and hepatocellular carcinoma.

Si306 is a Src inhibitor with antitumor activity. Si306 reduces the phosphorylation of focal adhesion kinase (FAK) and the expression of epidermal growth factor receptor (EGFR), and inhibits the invasion of human glioblastoma (GBM).

FAK-IN-10 is an inhibitor of FAK with an IC₅₀ of 76.3 μM. FAK-IN-10 exhibits antitumor activity against MCF-7 and A431 cell lines with IC₅₀s of 4.23 and 0.78 μM,respectively.

PF-562271 mesylate (VS-6062 mesylate) is an orally active, ATP-competitive, reversible FAK/Pyk2 inhibitor, with an IC₅₀ of 1.5 nM for FAK and 13 nM for Pyk2. PF-562271 mesylate induces tumor regression, and inhibits tumor growth, invasion and metastasis. PF-562271 mesylate exerts no effect on tumor necrosis, angiogenesis or apoptosis in an orthotopic mouse model of pancreatic ductal adenocarcinoma. When combined with Sunitinib (HY-10255A), PF-562271 mesylate reduces tumor vascularization, decreases serum alpha-fetoprotein levels and improves cachexia. PF-562271 mesylate can be used in research related to prostate cancer, breast cancer, pancreatic cancer, colon cancer, glioblastoma, lung cancer, pancreatic ductal adenocarcinoma and hepatocellular carcinoma.

Defactinib (Standard) is the analytical standard of Defactinib. This product is intended for research and analytical applications. Defactinib (VS-6063; PF-04554878) is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities.

Keracyanin (chloride) (Standard) is the analytical standard of Keracyanin (chloride). This product is intended for research and analytical applications. Keracyanin chloride inhibits NF-κB/FAK/MAPK signaling pathway. Keracyanin chloride exhibits antioxidant, anti-inflammatory and hypoglycemic effects, and is orally active.