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Beschreibung

A cell-permeable pyrazolopyrimidinylamino compound that acts as a potent, ATP-competitive and reversible inhibitor of CKIepsilon with ~22-fold greater potency over CKIdelta (IC50 = 32 and 711 nM, respectively) and displays excellent selectivity among 50-kinases, with the only exception of EGFR (69% inhibition at 1 µ,M). Shown to preferentially block PER3 (PERIOD3) nuclear translocation in COS7-GFP-PER3-CKIepsilon cells over CKIdelta-transfected cells (IC50 = 0.13 and 2.65 µ,M, respectively), and PER2 degradation in COS7-GFP-PER2-CKIepsilon cells. Unlike Casein Kinase I Inhibitor II, PF-670462 (Cat. No. 218716), PF-4800567 exerts only marginal effect on circadian clock under similar conditions.