| Description | 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 shows inhibitory activity against CK1ε 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 (32 nM) has little effect on the circadian clock [1]. |
| In vivo | PF-4800567 (100 mg/kg, s.c.) is rapidly absorbed and distributed in plasma and brain of mice [1]. |
| Target activity | CK1ε:32 nM, CKIδ:711 nM |
| molecular weight | 359.81 |
| Molecular formula | C17H18ClN5O2 |
| CAS | 1188296-52-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/mL (166.76 mM) |
| References | 1. Walton KM, et al. Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. J Pharmacol Exp Ther. 2009 Aug;330(2):430-9. |