Erastin is a ferroptosis inducer. Erastin shows selective cytotoxicity, targeting cells expressing oncogenic mutants of RAS. Erastin exhibits the mechanism of ferroptosis induction related to ROS and iron-dependent signaling. Erastin inhibits voltage-dependent anion channels (VDAC2/VDAC3) and accelerates oxidation, leading to the accumulation of endogenous reactive oxygen species. Erastin also disrupts mitochondrial permeability transition pore (mPTP) with anti-tumor activity.
性状
Solid
体外研究(In Vitro)
Erastin (10 μM;24 小时) 触发异位子宫内膜间质细胞 (EESC) 的铁死亡,并在 9 小时时增加总 ROS 水平。Erastin 能够缩短 EESC 细胞中的线粒体长度并增加它的膜密度。Erastin (10 μM;9 小时) 降低铁相关蛋白的 mRNA 表达水平,例如 EESC 中的 FPN (铁输出蛋白)。 然而,Erastin 诱导的 EESCs 铁死亡能够被 FPN 的过表达显著抑制。Erastin (10 μM;24 小时) 在 HT-29 结直肠癌细胞中诱导线粒体通透性转换孔 (mPTP) 打开。 Erastin (30 μM;72 小时) 显著抑制 HT-29 结直肠癌细胞的生长。Erastin 诱导铁死亡的分子机制与调节铁或线粒体脂肪酸代谢的基因有关。包括核糖体蛋白 L8、铁反应元件结合蛋白 2 (IREB2)、ATP 合酶 F0 复合亚基 C3、柠檬酸合酶、四肽重复结构域 35 和酰基辅酶 A 合成酶家族成员 2 (ACSF2)。 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Erastin (40 mg/kg;腹腔注射;每 3 天一次,持续 2 周) 抑制小鼠子宫内膜异位症模型中的子宫内膜异位植入,表明 Erastin 通过触发铁死亡使异位病变消退。
Erastin (10 mg/kg、30 mg/kg;腹腔注射;每天一次,持续 4 周) 抑制 SCID 小鼠的 HT-29 异种移植物生长,在 30 mg/kg 治疗下具有更有效的疗效。 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Li Y, et al. Erastin induces ferroptosis via ferroportin-mediated iron accumulation in endometriosis. Hum Reprod. 2021 Mar 18;36(4):951-964. [2]. Huo H, et al. Erastin Disrupts Mitochondrial Permeability Transition Pore (mPTP) and Induces Apoptotic Death of Colorectal Cancer Cells. PLoS One. 2016 May 12;11(5):e0154605.
溶解度数据
In Vitro: DMSO : 12.5 mg/mL (22.85 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)配制储备液