ISRIB is a potent and selective PERK inhibitor with IC50 of 5 nM. ISRIB reverses the effects of eIF2α phosphorylation on translation and stress granule assembly.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 10 mM|
The small molecule ISRIB reverses the effects of eIF2α phosphorylation on translation and stress granule assembly.
Sidrauski C, et al. Elife. 2015 Feb 26;4. PMID: 25719440.
Pharmacological brake-release of mRNA translation enhances cognitive memory.
Sidrauski C, et al. Elife. 2013 May 28;2:e00498. PMID: 23741617.
|Related PERK Products|
GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM, 500-fold greater against a panel of 300 kinases.
GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed.
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