Piperazine erastin is an inducer of ferroptosis.1,2 It inhibits glutamate release in human CCF-STTG1 astrocytoma cells (IC50 = 0.8 ?M), indicating inhibition of the system xc- cystine/glutamate transporter, and decreases glutathione (GSH) levels in HT-1080 fibrosarcoma cells when used at a concentration of 10 ?M. Piperazine erastin inhibits the growth of BJeLR cells overexpressing the H-Ras activating mutation H-RasG12V (IC50 = 0.3 ?M).1 It increases hepatic mRNA expression of the gene encoding Cox-2 and prevents tumor formation in an HT-1080 mouse xenograft model when administered at a dose of 60 mg/kg.2
1.Larraufie, M.-H., Yang, W.S., Jiang, E., et al.Incorporation of metabolically stable ketones into a small molecule probe to increase potency and water solubilityBioorg. Med. Chem. Lett.25(21)4787-4792(2015) 2.Yang, W.S., SriRamaratnam, R., Welsch, M.E., et al.Regulation of ferroptotic cancer cell death by GPX4Cell156(1-2)317-331(2014)