An allosteric activator of GPX4
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PKUMDL-LC-101-D04 is an allosteric activator of glutathione peroxidase 4 (GPX4).1 It increases GPX4 activity to 150% of control levels when used at a concentration of 20 μM in a cell-free assay and at 61 μM in wild-type, but not Gpx4-/-, mouse embryonic fibroblast (MEF) extracts. PKUMDL-LC-101-D04 (200 μM) also reduces cholesterol hydroperoxide-induced MEF death.
|1. Li, C., Deng, X., Zhang, W., et al. Novel allosteric activators for ferroptosis regulator glutathione peroxidase 4. J. Med. Chem. 62(1), 266-275 (2019).
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