PF-4800567 是酪蛋白激酶 1ε (CK1ε) 的选择性抑制剂,IC50为 32 nM,对其选择性是对 CK1δ 的 20 倍,IC50为711 nM。
产品描述
PF-4800567 is a selective inhibitor of casein kinase 1ε (CK1ε; IC50 = 32 nM) with greater than 20-fold selectivity over CK1δ.
体外活性
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].
体内活性
PF-4800567 (100 mg/kg, s.c.) is rapidly absorbed and distributed in plasma and brain of mice [1].
Cas No.
1188296-52-7
分子式
C17H18ClN5O2
分子量
359.81
储存和溶解度
DMSO:70 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years