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Description: GSK2656157 (GSK-2656157) is a novel, potent, ATP-competitive and highly selective inhibitor of PERK (PRKR-like endoplasmic reticulum kinase or protein kinase R (PKR)-like endoplasmic reticulum kinase) enzyme with IC50 of 0.9 nM in cell-free assays, it has 500-fold greater activity against a panel of 300 kinases. Treatment of GSK2656157 causes an inhibition of PERK and decreases in the downstream substrates, including phospho-eIF2alpha, ATF4 and CHOP. The inhibition of PERK results in effects on de novo protein synthesis as shown in BxPC3 cells.
References: Cancer Res. 2013 Mar 15; 73(6):1993-2002.
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