Imidazole ketone erastin (IKE) is an inducer of ferroptosis. It has inhibition of the system Xc- cystine/glutamate transporter.

Human astrocytoma cells (CCF-STTG1) were used, which contain the system xc?.17 Following a 2 h incubation period, glutamate released into the medium was detected fluorometrically using glutamate oxidase, horseradish peroxidase, and Amplex UltraRed. Dramatic improvement of the half-maximal inhibitory constants (IC50) for system xc? inhibition was observed for IKE (IC50: 30 nM), compared to erastin and PE [1].

In a diffuse large B cell lymphoma (DLBCL) xenograft model, IKE exerted an antitumor effect by inhibiting system xc-, leading to glutathione depletion, lipid peroxidation, and the induction of ferroptosis biomarkers [2].

1801530-11-9

C35H35ClN6O5

655.15

IKE;Imidazole ketone erastin

[1]Larraufie MH, et al. Incorporation of metabolically stable ketones into a small molecule probe to increase potency and water solubility. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4787-4792. [2]Zhang Y, et al. Imidazole Ketone Erastin Induces Ferroptosis and Slows Tumor Growth in a Mouse Lymphoma Model. Cell Chem Biol. 2019 May 16;26(5):623-633.e9.

[1]Yan R, Xie E, Li Y, et al. The structure of erastin-bound xCT–4F2hc complex reveals molecular mechanisms underlying erastin-induced ferroptosis. Cell Research. 2022-32（7）P1-4

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