化合物ISRIB (trans-isomer) T6183

Product Introduction
Bioactivity


英文名: ISRIB (trans-isomer)

描述: ISRIB (trans-isomer) (ISRIB trans-isomer)是一种 PERK 的高效抑制剂，可有效逆转 eIF2α 磷酸化的作用，IC50值为 5 nM。

细胞实验: U2OS cells are plated on 96-well plates and left to recover overnight. Cells are treated with either with 2 μg/ml tunicamycin or 100 nM thapsigargin in the presence or absence of 100 nM ISRIB or with ISRIB alone for the indicated and the level of eIF2α phosphorylation is determined[1].

体外活性: ISRIB blocks production of endogenous ATF4, whereas XBP1 mRNA splicing and XBP1s production persisted. ISRIB prevents cells from re-establishing ER homeostasis by blocking signaling through the PERK branch of the UPR, and decreases the viability of cells that are subjected to ER-stress. [1]

体内活性: ISRIB shows favorable properties in pharmacokinetic profiling experiments and good bioavailability in vivo. ISRIB (0.25 mg/kg i.p.) increases long-term memory in mice by enhancing spatial and fear-associated learning. [1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 1.11 mg/mL (2.46 mM)


关键字: ISRIB (trans isomer) | PERK | ISRIB (trans-isomer) | Autophagy | ISRIB (transisomer) | PKR-like endoplasmic reticulum kinase | Apoptosis | Inhibitor | Protein kinase R-like endoplasmic reticulum kinase | inhibit

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