PF4800567

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-4800567 是酪蛋白激酶 1ε (CK1ε；IC50 = 32 nM) 的选择性抑制剂，选择性比 CK1δ 高 20 倍以上。

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.

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.

PF-4800567 (100 mg/kg, s.c.) is rapidly absorpted and distributed in plasma and brain of mice.

PF 4800567 | PF-4800567

Metabolic Enzyme/Protease

Casein Kinase

CK1ε

——

——

1188296-52-7

359.8

C17H18ClN5O2

>98% (HPLC)

DMSO: 70 mg/mL

Nc1ncnc2n(nc(COc3cccc(Cl)c3)c12)C1CCOCC1

——

(-20℃)

With Ice Pack

≥ 2 years