GSK2850163

Description: GSK2850163 is a novel and potent inhibitor of inositol-requiring enzyme-1 alpha (IRE1alpha) which can inhibit IRE1alpha kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively. Activation of the inositol-requiring enzyme-1 alpha (IRE1a) protein caused by endoplasmic reticulum stress results in the homodimerization of the N-terminal endoplasmic reticulum luminal domains, autophosphorylation of the cytoplasmic kinase domains, and conformational changes to the cytoplasmic endoribonuclease (RNase) domains, which render them functional and can lead to the splicing of X-box binding protein 1 (XBP 1) mRNA.

References: Molecular Pharmacology December 2015, 88 (6) 1011-1023.