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GSK2850163 hydrochloride is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.

GSK2850163 hydrochloride is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively. The increased autophosphorylation of IRE1α can be reduced in a dose-dependent manner by GSK2850163 hydrochloride. Increasing concentrations of GSK2850163 hydrochloride are capable of reducing the increased XBP 1 transcriptional activity. Two additional kinases are weakly inhibited by GSK2850163 hydrochloride: Ron (IC50=4.4 μM) and FGFR1 V561M (IC50=17 μM)[1].

[1]. Nestor O. Concha, et al. Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity. Molecular Pharmacology December 2015, 88 (6) 1011-1023.

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