| Identification | Back Directory | [Name]
4(3H)-Quinazolinone, 2-[[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]methyl]-3-[4-(1-methylethoxy)[1,1'-biphenyl]-3-yl]- | [CAS]
1695533-44-8 | [Synonyms]
Erastin2
4(3H)-Quinazolinone, 2-[[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]methyl]-3-[4-(1-methylethoxy)[1,1'-biphenyl]-3-yl]- | [Molecular Formula]
C36H35ClN4O4 | [MDL Number]
MFCD32867306 | [MOL File]
1695533-44-8.mol | [Molecular Weight]
623.14 |
| Chemical Properties | Back Directory | [Boiling point ]
807.0±75.0 °C(Predicted) | [density ]
1.26±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°,Cprotect from light | [solubility ]
DMF: 10 mg/ml; DMF:PBS (pH 7.2) (1:1): 0.25 mg/ml; DMSO: 1 mg/ml | [form ]
A crystalline solid | [pka]
5.05±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
Erastin2 is a ferroptosis inducer and an inhibitor of the system xc- 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. | [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). |
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