4(3H)-Quinazolinone, 2-[[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]methyl]-3-[4-(1-methylethoxy)[1,1'-biphenyl]-3-yl]-

Description

Erastin2 is a ferroptosis inducer and an inhibitor of the system x_c^- cystine/glutamate transporter.^1,2 It inhibits glutamate release in CCF-STTG1 cells (IC₅₀ = 0.0035 μM).² It induces cell death in HAP1 cells when used at a concentration of 5 μM, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 or deferoxamine .¹ Erastin2 also induces ferroptotic cell death in HT-1080 cells (EC₅₀ = 0.15 μM), an effect that can be blocked by the reducing agent β-mercaptoethanol (EC₅₀ = >20 μM).³ It increases lipid peroxidation in HT-1080 cells when used at a concentration of 1 μM.

Uses

Erastin2, an Erastin (HY-15763) analog, is a ferroptosis inducer and a potent, selective inhibitor of the system xc(-) cystine/glutamate transporter[1][2][3][4]

References

1. Cao, J.Y., Poddar, A., Magtanong, L., et al. A genome-wide haploid genetic screen identifies regulators of glutathione abundance and ferroptosis sensitivity Cell Rep. 26(6),1544-1556(2019).
2. Dixon, S.J., Patel, D.N., Welsch, M., et al. Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis Elife 3,e02523(2014).
3. Magtanong, L., Ko, P.-J., To, M., et al. Exogenous monounsaturated fatty acids promote a ferroptosis-resistant cell state Cell Chem. Biol. 26(3),420-432(2019).