A GPX4 inhibitor
GPX4 inhibitor 26a is an inhibitor of glutathione peroxidase 4 (GPX4).1 It inhibits GPX4 activity by 71.7% at 1 µM. GPX4 inhibitor 26a is cytotoxic to 4T1 and MCF-7 breast cancer cells and HT-1080 fibrosarcoma cells (IC50s = 0.78, 6.9, and 0.15 µM, respectively). It decreases intracellular glutathione (GSH) levels and induces lipid peroxidation and ferroptosis in 4T1 cells when used at a concentration of 5 µM. GPX4 inhibitor 26a (15 and 30 mg/kg) reduces tumor growth in a 4T1 mouse xenograft model.
1.Tiedt, R., Degenkolbe, E., Furet, P., et al.A drug resistance screen using a selective MET inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patientsCancer Res.71(15)5255-5264(2011)
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