| Description | PF-5006739 is an effective and selective inhibitor of CK1δ/ε (IC50s: 3.9 nM and 17.0 nM, respectively). PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity. PF-5006739 decreases opioid drug-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner. |
| Target activity | CK1:17.0 nM, CK1δ:3.9 nM |
| molecular weight | 419.45 |
| Molecular formula | C22H22FN7O |
| CAS | 1293395-67-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Wager TT, et al. Casein kinase 1δ/ε inhibitor PF-5006739 attenuates opioid drug-seeking behavior. ACS Chem Neurosci. 2014 Dec 17;5(12):1253-65. 2. Cunningham PS, et al. Targeting of the circadian clock via CK1δ/ε to improve glucose homeostasis in obesity.Sci Rep. 2016 Jul 21;6:29983. |