PF4800567

PF-4800567 is a selective inhibitor of casein kinase 1ε (CK1ε; IC50 = 32 nM) with greater than 20-fold selectivity over CK1δ. (In Vitro) :PF-4800567 is a potent and selective inhibitor of casein kinase 1 (CK1), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM) . PF-4800567 shows inhibitory activity against CK1 and CK1δ in whole cells, with IC50s of 2.65 and 20.38 μM, respectively. PF-4800567 (0.01-10 μM) blocks CK1 -mediated PER3 nuclear localization mediated by CK1 and suppresses PER2 degradation at 1 μM. In addition, PF-4800567 has little effect on the circadian clock at 32 nM. (In Vivo) :PF-4800567 (100 mg/kg, s.c.) is rapidly absorpted and distributed in plasma and brain of mice.