FAK Inhibitor

GZD-552 is a potent orally active FAK inhibitor with a human FAK IC₅₀ of 5.8 nM. GZD-552 suppresses FAK phosphorylation activation and downstream ERK signaling. GZD-552 induces apoptosis and G₂/M cell cycle arrest, and exhibits antiproliferative activities in glioblastoma multiforme cells. GZD-552 exhibits antitumor efficacy in mice xenograft model. GZD-552 can be used for the research of glioblastoma multiforme.

Creosol (Standard) (2-Methoxy-4-methylphenol (Standard)) is the analytical standard of Creosol (HY-W040971). This product is intended for research and analytical applications. Creosol (2-Methoxy-4-methylphenol) is an endogenous metabolite that acts as an important chemical intermediate and potential biofuel mainly derived from lignocellulosic biomass. Creosol is blood brain barrier penetrable.

FAK-IN-3 (Compound 36) is a potent inhibitor of focal adhesion kinase (FAK). FAK-IN-3 not only decreases migration and invasion of PA-1 cells, but also reduces expression of MMP-2 and MMP-9. FAK-IN-3 inhibits tumor growth and metastasis, and no obvious adverse effects. FAK-IN-3 has the potential for the research of ovarian cancer.

FAK-IN-4 (Compound 7d) is potential FAK inhibitor with anticancer activities. FAK-IN-4 induces cell apoptosis.

Antitumor agent-165 (Compound 10l) is a potent focal adhesion kinase (FAK) inhibitor. Antitumor agent-165 exhibits effective antiproliferative activity against CAPAN-1, PANC-1, PATU-T, SUIT-2, BxPC-3, PDAC-3 and PANC-1 GR with IC₅₀s in the range of 1.04-3.44 μM.

Ephemeranthol A is a phenanthrene compound with anticancer and anti-inflammatory activities. Ephemeranthol A exerts significant anti-inflammatory effects in macrophages by inhibiting the NF-κB and MAPK signaling pathways. Ephemeranthol A induces apoptosis and inhibits metastasis of lung cancer cells by suppressing the FAK/Akt signaling and EMT processes. Ephemeranthol A can be used for the research of acute and chronic inflammatory diseases and non-small cell lung cancer.

FAK-IN-26 is a BBB-penetrable Focal Adhesion Kinase (FAK) inhibitor (IC₅₀: 0.87 nM). FAK-IN-26 significantly suppresses tumor cell viability, cancer stem cell activity, and cell migration in A549 and SKOV-3 cell lines. FAK-IN-26 has potent anti-cancer activity in A549 and SKOV-3 tumor mice models with tumor inhibition rates of 59.15 % and 57.9 %.

MLK3-IN-1 (Compound 37) is a selective inhibitor for mixed-lineage protein kinase 3 (MLK3) with an IC₅₀ <1 nM. MLK3-IN-1 inhibits FAK with an IC₅₀ of 15.5 μM. MLK3-IN-1 exhibits good metabolic stability in mouse and human liver microsomes.

FAK-IN-18 is a focal adhesion kinase (FAK) inhibitor with an IC₅₀ of .84 nM. FAK-IN-18 can be used for the research of gastric cancer.

P2X7R antagonist-1 is an orally active P2X7 receptor antagonist with an IC₅₀ of 3.57 μM. P2X7R antagonist-1 inhibits the proliferation, invasion and metastasis abilities of cancer cells. P2X7R antagonist-1 downregulates the expression of FAK and MMP-9. P2X7R antagonist-1 suppresses tumor growth and metastasis in a mouse breast cancer model. P2X7R antagonist-1 promotes the activation of CD4 and CD8 T cells. P2X7R antagonist-1 can be used in breast cancer-related research.

FAK-IN-24 (Compound 9f) is a FAK inhibitor (IC₅₀: 0.815 nM). FAK-IN-24 induces DNA damage and apoptosis. FAK-IN-24 has anti-glioblastoma activity. FAK-IN-24 inhibits proliferation of glioblastoma cell lines U87-MG (IC₅₀ = 15 nM) and U251 (IC₅₀ = 20 nM). FAK-IN-24 inhibits tumor growth in U87-MG xenograft model.

1α-Hydroxyvitamin D5 (CARD-024) is a vitamin D analog with extremely low hypercalcemic effects. 1α-Hydroxyvitamin D5 effectively attenuates the pro-fibrotic response of colonic myofibroblasts to TGFβ and high-stiffness substrates by inhibiting the expression of αSMA, the phosphorylation of FAK, and the gene expression of MLCK and ET-1, while activating the anti-inflammatory pathway of IL-1β/COX-2. 1α-Hydroxyvitamin D5 can be used in research related to intestinal fibrosis associated with Crohn's disease.

Nitidine (chloride) (Standard) is the analytical standard of Nitidine (chloride). This product is intended for research and analytical applications. Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.

Ifebemtinib (tosylate) (BI-853520 (tosylate); IN-10018 (tosylate)) is a highly selective PTK2 kinase inhibitor. Ifebemtinib (tosylate) demonstrates anti-tumor activity. Ifebemtinib (tosylate) inhibits FAK autophosphorylation in prostate carcinoma cells. Ifebemtinib (tosylate) can inhibit spheroid formation and orthotopic tumor growth in vivo. Ifebemtinib (tosylate) can be studied in anticancer research such as solid tumors, breast cancer, and malignant pleural mesothelioma.

FAK-IN-17 is a focal adhesion kinase (FAK) inhibitor. FAK-IN-17 possesses anticancer activity against A549 and MDA-MB-231 cell lines with IC₅₀ values of 130 nM and 94 nM.

FAK-IN-21 (compound 9) is a FAK inhibitor with the IC₅₀ of 37.52 nM. FAK-IN-21 inhibits cell growth and the phosphorylation of FAK. FAK-IN-21 can be used for study of diffuse gastric cancer.

FAK-IN-28 is an orally active FAK inhibitor (IC₅₀ = 0.4 nM). FAK-IN-28 exhibits dual antiproliferative and anti-metastatic properties. FAK-IN-28 triggers caspase-3-dependent apoptosis via ROS elevation. FAK-IN-28 inhibits tumor growth without causing weight loss or hepatotoxicity. FAK-IN-28 is useful in the study of FAK-driven malignancies, such as colon cancer, cervical cancer, triple-negative breast cancer, and melanoma.

FAK ligand-5 is a FAK ligand. FAK ligand-5 can be coupled with a linker to synthesize BI-4464 (HY-124625). FAK ligand-5 can be used as a target protein ligand for PROTAC development, specifically for designing PROTAC FAK degraders. FAK ligand-5 can be used in the synthesis of PROTAC FAK degrader 4 (HY-178467). FAK ligand-5 can be used in cancer research.

EGFR T790M/FAK-IN-2 is an orally active dual FAK and EGFR^T790M kinase inhibitor, with an IC₅₀ of 1.03 nM against FAK and an IC₅₀ of 3.89 nM against EGFR^T790M. EGFR T790M/FAK-IN-2 exerts antiproliferative effects in drug-resistant cancer cells overexpressing FAK, inducing apoptosis and cell cycle arrest. EGFR T790M/FAK-IN-2 exhibits antitumor activity in a pancreatic cancer xenograft mouse model. EGFR T790M/FAK-IN-2 can be used for the research of pancreatic cancer, breast cancer and non-small cell lung cancer.

STK899704 is a tubulin polymerization inhibitor. STK899704 exhibits broad-spectrum inhibitory activity against various cancer cell lines with IC₅₀ values ​​ranging from 0.2 to 1.0 μM. STK899704 disrupts the mitotic spindle structure, inducing G2/M phase cell cycle arrest. STK899704 inhibits the migration ability of HT29 cells by downregulating the FAK-MEK-ERK signaling pathway, thereby suppressing the expression and activity of MMP-2 and MMP-9. STK899704 activates caspase-3/7/8/9, leading to PARP cleavage and inducing apoptosis. STK899704 induces cellular senescence through the p53 pathway. STK899704 can be used in research on skin cancer, lung cancer, colon cancer, and other cancers.