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Experimental drugs
Erastin
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    Erastin

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    Erastin
    Erastin Structure.svg
    Legal status
    Legal status
    • Experimental
    Identifiers
    • 2-[1-[4-[2-(4-Chlorophenoxy)acetyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)-4(3H)-Quinazolinone
    CAS Number
    PubChem CID
    ChemSpider
    KEGG
    Chemical and physical data
    Formula C30H31ClN4O4
    Molar mass 547.05 g·mol−1
    3D model (JSmol)
    • O=C1N(C2=CC=CC=C2OCC)C(C(C)N3CCN(C(COC4=CC=C(Cl)C=C4)=O)CC3)=NC5=CC=CC=C51
    • InChI=1S/C30H31ClN4O4/c1-3-38-27-11-7-6-10-26(27)35-29(32-25-9-5-4-8-24(25)30(35)37)21(2)33-16-18-34(19-17-33)28(36)20-39-23-14-12-22(31)13-15-23/h4-15,21H,3,16-20H2,1-2H3
    • Key:BKQFRNYHFIQEKN-UHFFFAOYSA-N

    Erastin is a small molecule capable of initiating ferroptotic cell death. Erastin binds and activates voltage-dependent anion channels (VDAC) by reversing tubulin's inhibition on VDAC2 and VDAC3, and functionally inhibits the cystine-glutamate antiporter system Xc−. 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.

    Erastin was first described in 2003. Its name is short for "eradicator of RAS and ST-expressing cells".



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