Chemistry:Erastin

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Erastin
Erastin.png
Legal status
Legal status
  • Experimental
Identifiers
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC30H31ClN4O4
Molar mass547.05 g/mol g·mol−1
3D model (JSmol)

Erastin is a small molecule capable of initiating ferroptotic cell death.[1] Erastin binds and inhibits VDAC2 and VDAC3[2] and functionally inhibits the cystine-glutamate antiporter System Xc-.[3] Cells treated with erastin are deprived of cysteine and are unable to synthesize the antioxidant glutathione. Depletion of glutathione eventually leads to excessive lipid peroxidation and cell death.

References

  1. Dixon, SJ; Lemberg, KM; Lamprecht, MR; Skouta, R; Zaitsev, EM; Gleason, CE; Patel, DN; Bauer, AJ et al. (25 May 2012). "Ferroptosis: an iron-dependent form of nonapoptotic cell death.". Cell 149 (5): 1060–72. PMID 22632970. 
  2. Yagoda, N; von Rechenberg, M; Zaganjor, E; Bauer, AJ; Yang, WS; Fridman, DJ; Wolpaw, AJ; Smukste, I et al. (14 June 2007). "RAS-RAF-MEK-dependent oxidative cell death involving voltage-dependent anion channels.". Nature 447 (7146): 864–8. PMID 17568748. 
  3. Dixon, SJ; Patel, DN; Welsch, M; Skouta, R; Lee, ED; Hayano, M; Thomas, AG; Gleason, CE et al. (20 May 2014). "Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis.". eLife 3: e02523. PMID 24844246.