Imidazole ketone erastinImidazole ketone erastin
MedChemExpress (MCE)
HY-114481
1801530-11-9
IKE
99.77%
4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months
-20°C, 1 month (sealed storage, away from moisture and light)
Room temperature in continental US
may vary elsewhere.
Imidazole ketone erastin is a potent, selective, and metabolically stable inhibitor of the cystine-glutamate antiporter, system xc- and an activator of ferroptosis. Imidazole ketone erastin has anti-tumor activity.
Imidazole ketone erastin (IKE) (0.1 nM-100 μM
24 h) potently reduces diffuse large B cell lymphoma (DLBCL) cell number by lipid peroxidation and ferroptosis[1].IKE (1-250 nM
24 h) depletes reduced glutathione (GSH) in a dose-dependent manner with an IC50 of 34 nM in SUDHL6 cells[1].IKE (125-500 nM) increases lipid ROS in a dose-dependent manner in SUDHL-6 cells[1].IKE (500 nM
5-360 min) increases the system xc component SLC7A11, prostaglandin-endoperoxide synthase 2 (PTGS2), and ChaC glutathione-specific gamma-glutamylcyclotransferase 1 (CHAC1) expression in SUDHL-6 cells[1].IKE (500 nM and 1 μM) changes the relative abundance of 62 lipid species including lysophosphatidylcholines (LPC), phosphatidylcholines (PC), phosphatidylethanolamines (PE), and triglycerides (TAGs) in SUDHL6 cells[1].IKE (500 nM) activates de novo lipid biosynthesis pathways, phospholipid remodeling pathways, and arachidonic acid oxidation pathways in SUDHL6 cells[1].
IKE (23-40 mg/kg
i.p. once daily for 13 d) inhibits tumor growth in mice[1].IKE (50 mg/kg
a single i.p) depletes GSH significantly starting from 4 h, and increases in the relative abundance of free fatty acids, phospholipids, and diacylglycerols (DAG) in mice[1].IKE (50 mg/kg) exhibits half-life (1.82, 1.31, and 0.96 h) and Cmax (19515, 11384, and 5203 ng/mL) following different administration (i.p., i.v., and p.o. respectively) in mice[1].
System Xc-, ferroptosis[1] Cellular Effect Cell Line Type Value Description References
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[1]. Zhang Y, et al. Imidazole Ketone Erastin Induces Ferroptosis and Slows Tumor Growth in a Mouse Lymphoma Model. Cell Chem Biol. 2019 Jan 31. pii: S2451-9456(19)30030-3. [Content Brief]