Biochem/physiol Actions

Primary TargetPERK

Cell permeable: yes

General description

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.Please note that the molecular weight for this compound is batch-specific due to variable water content.

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.

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Pytel, D., et al. 2014. J. Biomol. Screen.19, 1024.

Packaging

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)