A cell-permeable tri-substituted imidazole compound that acts as a potent and reversible inhibitor of casein kinase Iε/δ (IC₅₀ = 7.7 and 14 nM, respectively) with modest to excellent selectivity over EGFR and p38 MAPK (IC₅₀ = 150 and 190 nM, respectively) and over 43 related kinases (IC₅₀ >0.3 to 30 µM), and a panel containing 116-receptors, transporters and other enzymes. Shown to inhibit PER3 nuclear translocation in GFP-PER3 and CKIε-cotransfected COS7 cells (EC₅₀ = 290 nM), and induce phase delays in circadian rhythms of monkeys & rats model (10 - 100 mg, s.c.); further, attenuate the locomotor stimulant response to methamphetamine.

Packaged under inert gas

Soluble in DMSO (<100 mM) or H2O ( <100 mM); aliquot & store at -20*C; stable for 6 months. Most likely to compete with ATP.

Bryant, C.D., et al. 2009. Psychopharmacology203, 703.
Sprouse, J., et al. 2009. Psychopharmacology204, 735.
Badura, L., et al. 2007. J. Pharmacol. Exp. Ther.322, 730.

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

Toxicity: Standard Handling (A)