| Name | ISRIB (trans-isomer) |
| Description | 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. |
| Cell Research | 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]. |
| In vitro | 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] |
| In vivo | 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] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+90% Saline : 0.11 mg/mL (0.24 mM), Solution.
DMSO : 1.11 mg/mL (2.46 mM), Sonication is recommended.
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| Keywords | Protein kinase R-like endoplasmic reticulum kinase | PKR-like endoplasmic reticulum kinase | PERK | ISRIB (trans-isomer) | ISRIB (transisomer) | ISRIB (trans isomer) | Autophagy | Apoptosis |
| Inhibitors Related | Stavudine | Aceglutamide | Hemin | Urea | Tamoxifen | Guanidine hydrochloride | Hydroxychloroquine | Metronidazole | Formamide | Paeonol | Naringin | Alginic acid |
| Related Compound Libraries | Highly Selective Inhibitor Library | Reprogramming Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Endoplasmic Reticulum Stress Compound Library | Kinase Inhibitor Library | Anti-Obesity Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Human Metabolite Library |
United States
