FAK Inhibitor

Defactinib-d6 is a deuterium labeled Defactinib (HY-12289). Defactinib is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities.

Vernodalin is an orally active, cytotoxic sesquiterpene lactone with a K_d value of 9.55 μM for p38 MAPK. Vernodalin downregulates the expression of phosphorylated ERK, JNK, AKT, PI3K, mTOR, p38MAPK, FAK, MMP-2, MMP-9, and uPA, while upregulates the expression of TIMP-1 and TIMP-2. Vernodalin increases ROS production, upregulates the expression of Bax and caspase 3, downregulates the expression of Bcl-2, and induces apoptosis (apoptosis), oxidative stress response and cell cycle arrest. Vernodalin inhibits the proliferation, adhesion and metastasis of cancer cells. Vernodalin enhances the activity of VEGF-B, AMPK and eNOS signaling pathways. Vernodalin alleviates myocardial injury and restores hemodynamic parameters. Vernodalin inhibits the growth of Trypanosoma brucei rhodesiense. Vernodalin can be used in research related to various cancers including gastric cancer, colorectal cancer and lung cancer, as well as African human trypanosomiasis and myocardial infarction.

Multi-kinase-IN-7 is a multikinase inhibitor with IC₅₀s of 2.19, 2.95, 3.59 and 9.31 μM against EGFR, VEGFR2, TrKA and CDK2, respectively. Multi-kinase-IN-7 shows moderate and weaker activity against FAK, AKT1, GSK3β and CDK5 with IC₅₀ values of 6.3, 9.2, 11.7 and 23.4 μM, respectively. Multi-kinase-IN-7 displays broad spectrum anti­proliferative potential against NCI cancer cell lines. Multi-kinase-IN-7 induces cell cycle arrest, apoptosis and necrosis. Multi-kinase-IN-7 Inhibitor can be used for the study of breast cancer.

GZD-257 is a brain-penetrant, ATP-competitive FAK inhibitor (IC₅₀ = 14.3 nM), performing 4.77-fold selectivity with FAK to Pyk2 (IC₅₀ = 68.2 nM). GZD-257 can significantly induce apoptosis of U118MG cells and arrest the cell cycle at the G2/M phase. GZD-257 can be used for the study of Glioblastoma (GBM).

Fangchinoline (Standard) is the analytical standard of Fangchinoline. This product is intended for research and analytical applications. Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing. Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK. Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer.

Chloropyramine hydrochloride (Standard) is the analytical standard of Chloropyramine hydrochloride. This product is intended for research and analytical applications. Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.

PROTAC FAK degrader 5 is a potent PROTAC degrader targeting FAK, with a DC₅₀ of 11.65 nM. PROTAC FAK degrader 5 induces FAK protein degradation, selectively inhibits colony formation of human colorectal cancer HCT116 cells, and blocks the proliferation of human umbilical vein endothelial HUVEC cells, exhibiting anti-angiogenic activity. PROTAC FAK degrader 5 can be used in the research of colorectal cancer and angiogenesis.

FAK-IN-29 is a selective FAK inhibitor with an IC₅₀ of 0.5 nM. FAK-IN-29 can inhibit the proliferation and colony formation of MDA-MB-231 cells, and induce cell cycle arrest and apoptosis. FAK-IN-29 exhibits antitumor activity and can be used for the research of tumors such as triple-negative breast cancer.

FAK-IN-9 (Compound 8f) is a potent and orally active FAK inhibitor with an IC₅₀ of 27.44 nM. FAK-IN-9 induces triple-negative breast cancer (TNBC) cell apoptosis.

COX/5-LO-IN-2 is a COX2, EGFR, COX1, 5-LOX, BRAF and FAK inhibitor with IC₅₀ of 1.22 μM, 2.5 μM, 2.95 μM, 4.65 μM, 7.4 μM, 12.2 μM, respectively. COX/5-LO-IN-2 induces cell growth arrest at G2/M phase. COX/5-LO-IN-2 triggers apoptotic activity by up-regulating proapoptotic proteins p53, Bax, and caspase-7 and down-regulating anti-apoptotic protein Bcl-2. COX/5-LO-IN-2 can be used for the research of breast cancer.

FAK-IN-27 (compound 8A) is a potent and selective FAK inhibitor with an IC₅₀ of 4.968 nM. FAK-IN-27 suppresses H1299 cells proliferation with an IC₅₀ of 0.28 μM. FAK-IN-27 can be used in the study of NSCLC.

FAK-IN-33 is a potent focal adhesion kinase (FAK) inhibitor with an IC₅₀ value of 10.23 nM against FAK. FAK-IN-33 inhibits the viability of U118-MG glioblastoma cells with an IC₅₀ of 0.29 μM, and shows low cytotoxicity toward LO2 and 2BS cells. FAK-IN-33 can be used in studies related to glioblastoma.

FAK-IN-12 (Compound 12S) is a FAK inhibitor (IC₅₀ = 47 nM). FAK-IN-12 inhibits MGC-803, HCT-116 and KYSE30 cell proliferation (IC₅₀: 0.24, 0.45, 0.44 μM). FAK-IN-12 induces apoptosis and cellular senescence.

Creosol-d₄ (2-Methoxy-4-methylphenol-d₄) is the deuterium labeled Creosol (HY-W040971). 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-11 (Compound 4l) is a FAK inhibitor. FAK-IN-11 binds to the ATP binding pocket of FAK, and inhibits phosphorylation of FAK protein. FAK-IN-11 shows cytotoxic activity against the MDA-MB-231 cells with an IC₅₀ of 13.73? μM. FAK-IN-11 induces non-apoptotic cell death in MDA-MB-231 cells.

FAK inhibitor 7 is a type of FAK inhibitor with an IC₅₀ value of 3.58 nM. FAK inhibitor 7 can inhibit the downstream signaling cascades of FAK (like Src and AKT), causing ovarian cancer cells to stall in the G0/G1 phase and induce cytotoxic autophagy. FAK inhibitor 7 can also suppress tumor metastasis and growth in ovarian cancer mice.

FAK-IN-6 is a potent FAK inhibitor with an IC₅₀ value of 1.415 nM. FAK-IN-6 has anti-proliferative activity against certain cancer cell lines. FAK-IN-6 can be used for researching pancreatic cancer.

ZINC09875266 is a dual inhibitor targeting VEGFR2 and FAK that can be used in cancer research.

FAK-IN-31 is a FAK inhibitor with antiproliferative activity against a variety of cancer cell lines. FAK-IN-31 serves as a PROTAC target protein ligand for the development of FAK-targeted PROTAC degrader heads, such as PROTAC FAK degrader 5 (HY-183768). FAK-IN-31 can be used in the research of colorectal cancer, pancreatic cancer, breast cancer, hepatocellular carcinoma and lung cancer.

PROTAC CYP1B1 degrader-2 is a CYP1B1 PROTAC degrader with a DC₅₀ of approximately 0.1 nM. PROTAC CYP1B1 degrader-2 induces ubiquitination and proteasomal degradation of CYP1B1, and forms a ternary complex with VHL ubiquitin ligase and CYP1B1. PROTAC CYP1B1 degrader-2 inhibits P-gp. PROTAC CYP1B1 degrader-2 inhibits FAK/SRC. PROTAC CYP1B1 degrader-2 exhibits anticancer activity against paclitaxel (HY-B0015)-resistant non-small cell lung cancer. PROTAC CYP1B1 degrader-2 can be used in studies related to non-small cell lung cancer.