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Overview
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Background
Liproxstatin-1 is a potent inhibitor of ferroptosis with IC50 value of 22 nM [1].
Ferroptosis is an iron-dependent non-apoptotic form of cell death induced by small molecules in engineered cells overexpressing oncogenic RAS and specific tumour types [1].
Liproxstatin-1 is a potent ferroptosis inhibitor. Liproxstatin-1 showed inhibition against ferroptosis-inducing agent (FIN) -triggered cell death. In Gpx4-/- cells, liproxstatin-1 inhibited RSL3-induced BODIPY 581/591 C11 oxidation. In primary human renal proximal tubule epithelial cells (HRPTEpiCs), liproxstatin-1 inhibited RSL3-induced cell death. Knock down Gpx4 in the immortalized human renal proximal tubule epithelial cell line (HK-2) cells made cells more sensitive to FIN [1].
On TAM treatment of CreERT2; Gpx4fl/fl mice, liproxstatin-1 significantly extended survival time and reduced number of TUNELC cells, which suggested that liproxstatin-1 delayed ferroptosis in tubular cells. In a hepatic ischaemia/reperfusion injury model, liproxstatin-1 mitigated tissue injury induced by ischaemia/reperfusion [1].
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- Properties
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Overview