Erastin - Ferroptosis Inducer - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEErastinCat. No.: HY-15763CAS No.: 571203-78-6分式: CHClNO分量: 547.04作靶点: Ferroptosis作通路: Apoptosis储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 6.4 mg/mL (11.70 mM; Need ultrasonic)Mass Solv

2、ent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.8280 mL 9.1401 mL 18.2802 mL5 mM 0.3656 mL 1.8280 mL 3.6560 mL10 mM 0.1828 mL 0.9140 mL 1.8280 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Erastin铁诱导的细胞死亡 (ferroptosis) 诱导剂。Erastin 结合且抑制电压依赖性 离通道 (VDAC2/VDAC3)。体外研究Erastin triggers

3、oxidative, iron-dependent cell death. Treatment of NRAS-mutant HT-1080 fibrosarcoma cellswith the RSL molecule erastin (10 M) results in a time-dependent increase in cytosolic and lipid ROSbeginning at 2 hours 1. Cell death triggered by erastin is significantly inhibited by antioxidants (e.g., -toco

4、pherol, butylated hydroxytoluene, and -carotene) and iron chelators, suggesting that ROS- and iron-1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEdependent signaling is required for erastin-induced ferroptosis. Erastin can directly bind to VDAC2/3 inBJeLR cells. Knockdown of VDAC2 and VDAC3, but n

5、ot VDAC1, leads to erastin resistance. Erastin has theability to reduce glutathione level by directly inhibiting cystine/glutamate antiporter system Xc activity, withactivation of the ER stress response 2. Erastin potently inhibits HT-29 cell survival. Erastin shows a dose-dependent effect, and 30 M

6、 of erastin displays the most dramatic effect 3.体内研究 Intraperitoneal injection of erastin at well-tolerated doses dramatically inhibits HT-29 xenograft growth insevere combined immunodeficient mice 3.PROTOCOLCell Assay 3 To test erastins activity on colorectal cancer cell survival, HT-29 cells are t

7、reated with increasingconcentrations of erastin (0.130 M). MTT assay was performed 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Mice are treated daily with 10 or 30 mg/kg body weight of erastin (intraperitoneal injection, for 4 weeks)A

8、dministration 3 or vehicle control (Saline). Tumor volumes are calculated. Mice body weights are also recorded every week3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Cell Death Dis. 2019 Apr 15;10(5):331. Biomater Sci. 2019 Jun 18. Cell

9、 Signal. 2019 Aug 5:109384. Commun Biol. (2018) 1:210See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Dixon SJ, et al. Ferroptosis: an iron-dependent form of nonapoptotic cell death. Cell. 2012 May 25;149(5):1060-72.2. Xie Y, et al. Ferroptosis: process and function. Cell Death Differ. 2016 Mar;23(3):369-79.3. Huo H, et al. Erastin Disrupts Mitochondrial Permeability Transition Pore (mPTP) and Induces Apoptotic Death of Colorectal CancerCells. PLoS One. 2016 May 12;11(5):e0154605.McePdfHeightCaution: Product has not been fully validated