erastin

Erastin is a synthetic small molecule that acts as a potent and selective inducer of ferroptosis, an iron-dependent form of regulated cell death distinct from apoptosis. It exerts its effect primarily by inhibiting the cystine-glutamate antiporter system Xc− (specifically binding to SLC7A11), leading to depletion of intracellular cysteine and glutathione, which results in excessive lipid peroxidation and cell death. Erastin also binds to and activates voltage-dependent anion channels (VDAC2/VDAC3) on mitochondria, reversing tubulin-mediated inhibition. This dual action disrupts redox homeostasis in cells, particularly those with oncogenic RAS mutations or altered metabolic states, making it a valuable tool compound for studying ferroptosis in cancer biology and other diseases such as neurological disorders and acute kidney injury[1][2][5][8]. Erastin is widely used in research but has poor metabolic stability and solubility in vivo; thus, it is not approved for clinical use[8].

Other names

2-[1-[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)-4(3H)-quinazolinoneCHEBI:94287571203-78-6