产品描述:
ML-162 is an inhibitor of glutathione peroxidase 4 (GPX4) and thioredoxin reductase 1 (TrxR1).{57628} It covalently binds to the GPX4 active site residue selenocysteine 46 (Sec46) and allosteric site residue Cys66 but does not inhibit recombinant human GPX4 activity in a cell-free assay.{66811,55163,64989} ML-162 inhibits TrxR1 in a cell-free assay (IC50 = 19.5 µM) and in A549 cells when used at concentrations ranging from 0.5 to 15 µM.{64989} ML-162 (10 µM) induces the accumulation of cellular lipid hydroperoxides, a marker of ferroptosis, in LOX-IMVI human melanoma cells, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 (Item No. 17729).{55163} It decreases GPX4 levels in MDA-MB-231 breast cancer cells and reduces the viability of BT-549 breast cancer cells, an effect that can be enhanced by α-eleostearic acid (9(Z),11(E),13(E)-octadecatrienoic acid; Item No. 10008349). ML-162 also selectively induces Ras-synthetic lethality in mutant RAS oncogene-expressing cells (IC50s = 25 and 578 nM for HRASG12V-expressing and wild-type RAS-expressing BJeH cells, respectively).{33150}