A cell-permeable tricyclic heterocycle oxime that acts as a reversible and non ATP-competitive inhibitor of PERK (PKR-like ER kinase, IC50 = 7.04 µM) and blocks PERK-dependent phosphorylation of elF2a. Shown to reduce thapsigargin-induced elF2a phosphorylation in mouse embryonic fibroblasts over a wide range. Does not exhibit any cellular toxicity up to 50 µM levels.
A cell-permeable, reversible, and non ATP-competitive inhibitor of PERK (PKR-like ER kinase, IC₅₀ = 7.04 µM) and blocks PERK-dependent phosphorylation of elF2a.