PF-5006739 is a potent, selective casein kinase CK1δ/ε inhibitor with IC50 of 3.9/17.0 nM, respectively.
PF-5006739 demonstrates excellent kinome selectivity in a 59-kinase panel with exception of JNK2 (IC50=6.1 uM) and ZC3 (IC50=1.5 uM).
PF-5006739 exhibits robust centrally mediated circadian rhythm phase-delaying effects in both nocturnal and diurnal animal models, attenuates opioid drug-seeking behavior in a rodent operant reinstatement model in animals trained to self-administer fentanyl.
PF-5006739 also improves glucose tolerance in both DIO and genetic (ob/ob) models of obesity.
