isrib-trans-isomer

Description: ISRIB, the trans-isomer of ISRIB, is a novel, potent and selective inhibitor of PERK (PRKR-like endoplasmic reticulum kinase or protein kinase R (PKR)-like endoplasmic reticulum kinase) with IC50 of 5 nM. ISRIB reversed the effects of eIF2alpha phosphorylation with IC50 value of 5 nM. ISRIB inhibited production of endogenous ATF4 (a cAMP element binding transcription factor). In mouse embryonic fibroblasts (MEFs), ISRIB reversed the increase in the 80S monosomes at the expense of polyribosomes induced by endoplasmic reticulum (ER) stress. In ER-stressed cells, ISRIB reduced cell survival. In stressed cells, ISRIB restored mRNA translation and inhibited stress granule (SG) formation induced by eIF2alpha phosphorylation.

References: Science. 2015 May 29; 348(6238):1027-30; Elife. 2015 Apr 15; 4:e07314.

Related CAS: 548470-11-7 (cis-isomer)