FerroLOXIN-1 is an inhibitor of the 15-lipoxygenase-2 (15-LO-2) and phosphatidylethanolamine-binding protein 1 (PEBP1) catalytic complex.[1] It selectively inhibits the peroxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-PE by the 15-LO-2/PEBP1 complex over 15-LO-2 alone in cell-free assays when used at a concentration of 0.25 µM. FerroLOXIN-1 inhibits RSL3-induced ferroptosis in primary human bronchial epithelial cells (IC50 = 84 nM). It increases survival in a mouse model of total body irradiation when administered at a dose of 25 mg/kg.
References:
[1].Dar, H.H., Mikulska-Ruminska, K., Tyurina, Y.Y., et al.Discovering selective antiferroptotic inhibitors of the 15LOX/PEBP1 complex noninterfering with biosynthesis of lipid mediatorPNAS120(25)e2218896120(2023).