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Erastin

Erastin 是一种铁死亡 (ferroptosis) 诱导剂。Erastin 的铁死亡诱导机制与 ROS 和铁依赖性信号传导有关。Erastin 能够抑制电压依赖性阴离子通道 (VDAC2/VDAC3),加速氧化,导致内源活性氧积累。Erastin 还破坏线粒体通透性过渡孔 (mPTP),表现出抗肿瘤活性。

  • 货号:
    TK0112
  • 规格:
    1mg
    5mg
  • 价格:
    0.00

产品参数

CAS No.571203-78-6
生物活性Erastin is a ferroptosis inducer. Erastin binds and inhibits voltage-dependent anion channels (VDAC2/VDAC3).
分子式C30H31ClN4O4
分子量547.04
运输条件Room temperature in continental US; may vary elsewhere.
储存条件Powder -20℃ 3 years
溶解性数据DMSO : 12.5 mg/mL (22.85 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble)
体内研究Intraperitoneal injection of erastin at well-tolerated doses dramatically inhibits HT-29 xenograft growth in severe combined immunodeficient mice.
体外研究Erastin triggers oxidative, iron-dependent cell death. Treatment of NRAS-mutant HT-1080 fibrosarcoma cells with the RSL molecule erastin (10 µM) results in a time-dependent increase in cytosolic and lipid ROS beginning at 2 hours. Cell death triggered by erastin is significantly inhibited by antioxidants (e.g., α-tocopherol, butylated hydroxytoluene, and β-carotene) and iron chelators, suggesting that ROS- and iron-dependent signaling is required for erastin-induced ferroptosis. Erastin can directly bind to VDAC2/3 in BJeLR cells. Knockdown of VDAC2 and VDAC3, but not VDAC1, leads to erastin resistance. Erastin has the ability to reduce glutathione level by directly inhibiting cystine/glutamate antiporter system Xc− activity, with activation of the ER stress response. Erastin potently inhibits HT-29 cell survival. Erastin shows a dose-dependent effect, and 30 μM of erastin displays the most dramatic effect.
文献Lipin3 defciency promotes hepatocyte ferroptosis and pyroptosis via activating JAK1-STAT3 pathway during acetaminophen induced acute liver injury
纯度及产品资料98%
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