Imidazole ketone eRastin 是一种铁死亡的诱导剂。它对系统Xc-胱氨酸/谷氨酸转运蛋白具有抑制作用。

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

DMSO:100 mg/mL (152.64 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years