Erastin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Erastin 是一种铁死亡激活剂，通过作用于线粒体 VDAC，对携带致癌 RAS 的肿瘤细胞表现出选择性。

Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS.(In Vitro):Erastin (10 μM; 24 h) triggers ferroptosis in ectopic endometrial stromal cells (EESCs), and increases the total ROS level at 9 h.Erastin shorts mitochondria and increases membrane density in EESCs.Erastin (10 μM; 9 h) decreases the mRNA expression levels of iron-related proteins, such FPN (iron exporter) in EESCs. However, FPN overexpression significantly inhibits erastin-induced ferroptosis in EESCs.Erastin (10 μM; 24 h) induces mitochondrial permeability transition pore (mPTP) opening in HT-29 colorectal cancer cells.Erastin (30 μM; 72 h) significantly inhibits the growth of HT-29 colorectal cancer cells.The molecular mechanism by which Erastin induces ferroptosis is related to genes regulating iron or mitochondrial fatty acid metabolism. Includes ribosomal protein L8, iron response element binding protein 2 (IREB2), ATP synthase F0 complex subunit C3, citrate synthase, tetrapeptide repeat domain 35, and acyl-CoA synthetase family member 2 (ACSF2).(In Vivo):Erastin (40 mg/kg; i.p.; once every 3 days for 2 weeks) suppresses endometriotic implants in the mouse endometriosis model, indicating Erastin regresses ectopic lesions by trigging ferroptosis.Erastin (10 mg/kg, 30 mg/kg; i.p.; once daily.

Cell Viability Assay Cell Line:Normal endometrial stromal cells (NESCs) and endometrial stromal cells (EESCs)Concentration:0, 0.5, 0.8, 1, 1.5, 2, 2.5, 5, 10?μM Incubation Time:24 hours Result:Induced cell detachment and overt death in EESCs, but not NESCs.Apoptosis AnalysisCell Line:EESCs infected with adenovirus expressing FPN cDNA (co-incubation for 24 hr)Concentration:0, 0.5, 1.5, 2.5, 5 and 2.5?μM Incubation Time:24 hours Result:Induced ferroptosis by decreasing the levels of total ROS and lipid ROS. And reversed by the overexpression of FPN in adenovirus-infected cells.

Animal Model:Mouse model of endometriosisDosage:40 mg/kg Administration:Intraperitoneal injection; once every 3 days for 2 weeksResult:Showed little impact on body weight of mice and hair of mice displayed neat and glossy.

Erastin

Apoptosis

Ferroptosis

Ferroptosis

Cancer

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571203-78-6

547.04

C30H31ClN4O4

>98% (HPLC)

DMSO: 19 mg/mL (34.73 mM)

O=C1N(C2=CC=CC=C2OCC)C(C(N3CCN(C(COC4=CC=C(Cl)C=C4)=O)CC3)C)=NC5=C1C=CC=C5

2-(1-(4-(2-(4-chlorophenoxy)acetyl)piperazin-1-yl)ethyl)-3-(2-ethoxyphenyl)quinazolin-4(3H)-one

(-20℃)

With Ice Pack

≥ 2 years