(1S,3R)-RSL3

(1S,3R)-RSL3 is a ferroptosis inducer and is canonically known as an inhibitor of glutathione peroxidase 4 (GPX4).^1,2,3 It inhibits GPX4 in a context-dependent manner: (1S,3R)-RSL3 inhibits GPX4 in the presence of cell cytosol or recombinant human 14-3-3ε, 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.^4,5 (1S,3R)-RSL3 (50 nM) inhibits peroxidase activity in GPX4-overexpressing COH-BR1 breast cancer cell lysates.¹ It also inhibits thioredoxin reductase 1 (TrxR1; IC₅₀ = 7.9 µM in a cell-free assay).⁴ (1S,3R)-RSL3 is selectively cytotoxic to H-Ras^V12-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.^1,2 In vivo, (1S,3R)-RSL3 (100 mg/kg) prevents tumor formation and inhibits tumor growth in BJeLR mouse xenograft models.¹

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