1801530-11-9

Imidazole ketone erastin is an inducer of ferroptosis. It inhibits glutamate release in human CCF-STTG1 astrocytoma cells (IC₅₀ = 30 nM), indicating inhibition of the system x_c^- cystine/glutamate transporter. Imidazole ketone erastin increases production of lipid reactive oxygen species (ROS) in SUDHL6 diffuse large B cell lymphoma (DLBCL) cells in a concentration-dependent manner, as well as reduces glutathione (GSH) levels in these cells (IC₅₀ = 34 nM). It inhibits the growth of HT-1080 fibrosarcoma cells (GI₅₀ = 310 nM) as well as HRAS^G12V-overexpressing BJeLR cells (IC₅₀ = 3 nM). Imidazole ketone erastin (23 and 40 mg/kg) reduces tumor growth in an SUDHL6 mouse xenograft model.

PUN30119 is potent, metabolically stable inhibitor of system xc.

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[3] ZHIPENG LI. Ribosome stalling during selenoprotein translation exposes a ferroptosis vulnerability[J]. Nature chemical biology, 2022, 18 7: 751-761. DOI: 10.1038/s41589-022-01033-3