PF 4800567

PF 4800567化学性质

沸点 :592.9±50.0 °C(Predicted)
密度 :1.52±0.1 g/cm3(Predicted)
储存条件 :Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解度 :DMF: 25 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml; DMSO: 10 mg/ml; Ethanol: 1 mg/ml
形态 :A crystalline solid
酸度系数(pKa) :4.01±0.30(Predicted)
颜色 :Light yellow to yellow

PF 4800567性质、用途与生产工艺

生物活性 PF 4800567是casein kinase 1 epsilon (IC50=32 nM) 的新型有效抑制剂，其选择性是casein kinase 1 delta(IC50=711 nM)的20倍以上。
靶点
Target Value
casein kinase 1 epsilon
(Cell-free assay) 32 nM
casein kinase 1 delta
() 711 nM
体外研究

PF-4800567 is a potent and selective inhibitor of casein kinase 1ϵ (CK1ϵ), with an IC ₅₀ of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC ₅₀ , 711 nM). PF-4800567 shows inhibitory activity against CK1ϵ and CK1δ in whole cells, with IC ₅₀ s of 2.65 and 20.38 μM, respectively. PF-4800567 (0.01-10 μM) blocks CK1ϵ-mediated PER3 nuclear localization mediated by CK1ϵ and suppresses PER2 degradation at 1 μM. In addition, PF-4800567 has little effect on the circadian clock at 32 nM.
体内研究

PF-4800567 (100 mg/kg, s.c.) is rapidly absorpted and distributed in plasma and brain of mice.
用途
PF 4800567 is a selective casein kinase inhibitor; displays 22-fold greater potency towards CK1ε than CK1δ (IC50 values are 32 and 711 nM for CK1ε and CK1δ respectively). ATP competitive. Displays minimal effect on the circadian clock.

PF 4800567上下游产品信息

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PF 4800567 试剂级价格

PF 4800567生产厂家

Target	Value
casein kinase 1 epsilon (Cell-free assay)	32 nM
casein kinase 1 delta ()	711 nM