General description

A cell-permeable purine compound that acts as a reversible and ATP-competitive dual inhibitor of CKIα and CKIδ activities (IC₅₀ = 5.6 and 8.8 µM) with moderate selectivity over Cdk7 and Erk2 (IC₅₀ = 29 and 52 µM). Shown to block CKIα/δ-mediated phosphorylation of PER1, a clock protein, (IC₅₀ ~ 9 µM) and repress PER1 proteasomal degradation, and lengthen the circadian period in U2OS cells (by ~ 13 hrs at 10 µM) much more effectively than Casein Kinase I Inhibitor, D4476 (Cat. No. 218696) and IC261 (Cat. No. 400090) and in larval zebra fish.

Legal Information

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

Other Notes

Hirota, T., et al. 2010. PLoS Biol.8, e1000559.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Harmful (C)