| 名称 | ISRIB (trans-isomer) |
| 描述 | ISRIB (trans-isomer) is a potent inhibitor of PERK (IC50=5 nM) that restores protein translation and prevents SG formation in the presence of P-eIF2α. |
| 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 | METHODS: HEK293T cells were treated with clindamycin (2 µg/mL) to induce ER stress and with ISRIB (trans-isomer) or ISRIB (cis-isomer) (0-1 µM) for 7 h. The ATF4 fluorokinase reporter gene was detected.
RESULTS: ISRIB (trans-isomer) was 100-fold more potent (IC50=5 nM) than ISRIB (cis-isomer) (IC50=600 nM), suggesting that the compound interacts stereospecifically with its cellular target. [1]
METHODS: HEK293T cells were treated with Tm (1 µg/mL) and ISRIB (200 nM) for 1 h. Translation and mRNA changes were detected.
RESULTS: ISRIB completely blocked the translational changes that occurred under ER stress. A large number of genes with significant changes in expression upon stress collapsed to the center of the graph under ISRIB and Tm co-treatment. [2] |
| 体内活性 | METHODS: To investigate the effects on memory, ISRIB (0.25-2.5 mg/kg) was administered intraperitoneally to CD-1 mice.
RESULTS: ISRIB-treated mice showed significant enhancement in spatial and fear-related learning. [1] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | 10% DMSO+90% Saline : 0.11 mg/mL (0.24 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
DMSO : 1.11 mg/mL (2.46 mM), Sonication is recommended.
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| 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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| 相关库 | 高选择性抑制剂库 | 细胞重编程化合物库 | 经典已知活性库 | HIF-1化合物库 | 激酶抑制剂库 | 抑制剂库 | 抗衰老化合物库 | 已知活性化合物库 | 抗癌化合物库 | 人代谢物化合物库 |
United States
