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Ferristatin II is an inhibitor of iron uptake.1 It inhibits iron uptake (IC50 = ~12 µM), as well as induces degradation of transferrin receptor protein 1 (TfR1), an effect that can be reversed by the lipid membrane disruptor nystatin, in HeLa cells. In vivo ferristatin II (0.2, 10, and 40 mg/kg) reduces serum iron levels and transferrin saturation in rats. It also suppresses traumatic brain injury-induced lipid peroxidation, neuronal apoptosis, and the number of cortical iron deposits in rats.2
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1. Ferristatin II promotes degradation of transferrin receptor-
2. Ferristatin II, an iron uptake inhibitor, exerts neuroprotection against traumatic brain injury via suppressing ferroptosis. ACS Chem. Neurosci. 13(5), 664-675 (2022).