Fig. 5: PERK inhibitors of distinct chemotypes activate GCN2 and induce eIF2α phosphorylation in vitro.
From: Activation of the integrated stress response by inhibitors of its kinases
a Immunoblots of indicated proteins from in vitro kinase assays with 7.5 nM GCN2, 2 μM eIF2α, 12 μM ATP and increasing concentrations of GSK’414 or AMG44 PERK. 10 μM of the GCN2 inhibitor A92 was added in the indicated lanes. Active (A) and Inactive (I) GCN2 are indicated with arrows. Representative experiment from n = 2, biologically independent experiments. b, c Immunoblots of indicated proteins as in (a), from reconstituted in vitro kinase reactions with 12 μM ATP, with or without 0.04 μM A92 and with indicated concentrations of GSK’414 or AMG44. Active (A) and Inactive (I) GCN2 are indicated with arrows. Representative experiments from n = 2 (per compound), biologically independent experiments. Source data are provided as a Source data file.
