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FA16 is a ferroptosis inducer and an inhibitor of the system xc- cystine/glutamate transporter. It reduces the viability of various cancer cell lines, including HT-1080 fibrosarcoma and A375 melanoma cells (IC50s = 1.26 and 2.31 µM, respectively), 786-O renal cell carcinoma cells (IC50 = 0.7 µM), and MDA-MB-231 breast cancer cells (IC50 = 4.34 µM) but not several non-cancer cell lines at 20 µM. FA16-induced death of HT-1080 cells can be blocked by the ferroptosis inhibitors ferrostatin-1 (Cay-17729), Trolox (Cay-10011659), and deferoxamine (DFO, Cay-14595) and potentiated by ferric ammonium citrate or ferric citrate. FA16-induced death of HT-1080 cells can also be blocked by beta-mercaptoethanol, which prevents cell death induced by system xc- cystine/glutamate transporter inhibition by increasing intracellular cystine bioavailability. FA16 (5 µM) increases the production of reactive oxygen species (ROS) in HT-1080 cells, an effect that can be blocked by ferrostatin-1, and inhibits glutamate release from HT-1080 cells in an enzyme-coupled glutamate release assay. FA16 (15 and 30 mg/kg) reduces tumor growth and increases intratumoral levels of 4-hydroxy nonenal (4-HNE, Cay-32100) and malondialdehyde (MDA), markers of lipid peroxidation, in a HepG2 mouse xenograft model. It also has an increased half-life and slower clearance than the ferroptosis inducer erastin (Cay-17754) in human and rat liver microsomes.Formal Name: N,N-dimethyl-4-(4-((2-(trifluoromethyl)-1H-benzo[d]imidazol-1-yl)methyl)piperidin-1-yl)benzenesulfonamide. Molecular Formula: C22H25F3N4O2S. Formula Weight: 466.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Slightly soluble: 0.1-1 mg/ml, Ethanol: Slightly soluble: 0.1-1 mg/ml, PBS (pH 7.2): Slightly soluble: 0.1-1 mg/ml. SMILES: FC(F)(F)C1=NC2=CC=CC=C2N1CC3CCN(C4=CC=C(S(N(C)C)(=O)=O)C=C4)CC3. InChi Code: InChI=1S/C22H25F3N4O2S/c1-27(2)32(30,31)18-9-7-17(8-10-18)28-13-11-16(12-14-28)15-29-20-6-4-3-5-19(20)26-21(29)22(23,24)25/h3-10,16H,11-15H2,1-2H3. InChi Key: JIYXEVFXCPXAIH-UHFFFAOYSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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