ISRIB 是综合应激反应 (ISR) 的脑渗透抑制剂 |MedChemExpress (MCE)

CAS：548470-11-7

品牌：MedChemExpress (MCE)

存储条件：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

生物活性：ISRIB 是综合应激反应 (ISR) 的脑渗透抑制剂。ISR 的持续激活与几种神经系统疾病的发展有关，ISR 通过抑制 eIF2B 来抑制翻译。ISRIB 通过促进 eIF2B 的核苷酸交换活性和恢复翻译来抑制 ISR，因此可以用于神经系统疾病的研究。

体外：ISRIB (200 nM, 2 h) 阻断 U2OS 细胞 eIF2α 磷酸化诱导的应激颗粒形成[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：ISRIB (0.25 mg/kg，腹腔注射，每日) 可恢复朊病毒患病小鼠 eIF2α 磷酸化下游的翻译，对朊病毒患病小鼠具有神经保护作用[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考详情：ISRIB | 综合应激反应抑制剂 | MCE

 

参考文献：

[1]. Zyryanova AF, et al. ISRIB Blunts the Integrated Stress Response by Allosterically Antagonising the Inhibitory Effect of Phosphorylated eIF2 on eIF2B. Mol Cell. 2021 Jan 7;81(1):88-103.e6.

[2]. Halliday M, et al. Partial restoration of protein synthesis rates by the small molecule ISRIB prevents neurodegeneration without pancreatic toxicity. Cell Death Dis. 2015 Mar 5;6(3):e1672.[3]. Sidrauski C, et al. The small molecule ISRIB reverses the effects of eIF2α phosphorylation on translation and stress granule assembly. Elife. 2015 Feb 26;4:e05033.