(1S,3R)-RSL3

(1S,3R)-RSL3 is a ferroptosis inducer and is canonically known as an inhibitor of glutathione peroxidase 4 (GPX4). It inhibits GPX4 in a context-dependent manner: (1S,3R)-RSL3 inhibits GPX4 in the presence of cell cytosol or recombinant human 14-3-3epsilon, an adaptor protein, but does not inhibit recombinant human selenocysteine-containing GPX4 or purified rat testis GPX4, when used at a concentration of 100 µM. (1S,3R)-RSL3 (50 nM) inhibits peroxidase activity in GPX4-overexpressing COH-BR1 breast cancer cell lysates. It also inhibits thioredoxin reductase 1 (TrxR1, IC50 = 7.9 µM in a cell-free assay). (1S,3R)-RSL3 is selectively cytotoxic to H-RasV12-expressing BJeLR cells over wild-type Ras-expressing BJeH cells (EC50s = 0.01 and 2 µM, respectively) and induces lipid peroxidation, a hallmark of ferroptosis, in Pfa1 fibroblasts when used at a concentration of 100 nM. In vivo, (1S,3R)-RSL3 (100 mg/kg) prevents tumor formation and inhibits tumor growth in BJeLR mouse xenograft models.Formal Name: (1S,3R)-2-(2-chloroacetyl)-2,3,4,9-tetrahydro-1-[4-(methoxycarbonyl)phenyl]-1H-pyrido[3,4-b]indole-3-carboxylic acid, methyl ester. CAS Number: 1219810-16-8. Molecular Formula: C23H21ClN2O5. Formula Weight: 440.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml, Ethanol: 25 mg/ml. lambdamax: 220 nm. SMILES: O=C(OC)[C@@H]1N(C(CCl)=O)[C@@H](C2=CC=C(C(OC)=O)C=C2)C3=C(C(C=CC=C4)=C4N3)C1. InChi Code: InChI=1S/C23H21ClN2O5/c1-30-22(28)14-9-7-13(8-10-14)21-20-16(15-5-3-4-6-17(15)25-20)11-18(23(29)31-2)26(21)19(27)12-24/h3-10,18,21,25H,11-12H2,1-2H3/t18-,21+/m1/s1. InChi Key: TXJZRSRTYPUYRW-NQIIRXRSSA-N.