Description
Ferroptosis inducer [1]. Inhibits the cystine-glutamate antiporter, system Xc- leading to activation of an ER stress response [2]. Inhibition of system Xc- leads to cysteine starvation, glutathione depletion and induction of ferroptosis [3]. Also blocks mitochondrial voltage-dependent anion channels (specifically VDAC2 and 3) [4].
References:
1) Dolma et al. (2003), Identification of genotype-selective antitumor agents using synthetic lethal chemical screening in engineered human tumor cells; Cancer Cell, 3 285
2) Dixon et al. (2014), Pharmacological inhibition of cysteine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis; Elife, 3 e02523
3) Sato et al. (2018), The ferroptosis inducer erastin irreversibly inhibits system xc-and synergizes with cisplatin to increase cisplatin’s cytotoxicity in cancer cells; Sci. Rep., 8 968
4) Yagoda et al. (2007), RAS-RAF-MEK-dependent oxidative cell death involving voltage-dependent anion channels; Nature, 447 864
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For research use only. Not for diagnostic or clinical use.