GSK2656157

GSK2656157 is an inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK; IC₅₀ = 0.9 nM).^1,2 It is selective for PERK over a panel of additional kinases.¹ GSK2656157 blocks both stress-induced PERK autophosphorylation and eIF2α substrate phosphorylation and decreases levels of ATF4 and CHOP in multiple cell lines.¹ It is orally bioavailable, suppressing PERK autophosphorylation in mouse pancreas and inhibiting the growth of multiple human tumor xenografts in mice.^1,2 GSK2656157 inhibits caspase 1 activation in macrophage-like J774.1 cells, preventing LPS-induced IL-1β production, through its effects on the PERK/eIF2α pathway.³

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1. Atkins, C., Liu, Q., Minthorn, E., et al. Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res. 73(6), 1993-2002 (2013).

2. Axten, J.M., Romeril, S.P., Shu, A., et al. Discovery of GSK2656157: An optimized PERK inhibitor selected for preclinical development. ACS Med. Chem. Lett. 4, 964-968 (2013).

3. Ando, T., Komatsu, T., Naiki, Y., et al. GSK2656157, a PERK inhibitor, reduced LPIS-induced IL-1b production through inhibiting caspase 1 activation in macrophage-like J774.1 cells. Immunopharmacol. Immunotoxicol. 38(4), 298-302 (2016).