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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。
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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 160 | 现货 | |
5 mg | ¥ 398 | 现货 | |
10 mg | ¥ 648 | 现货 | |
25 mg | ¥ 1,390 | 现货 | |
50 mg | ¥ 2,070 | 现货 | |
100 mg | ¥ 2,950 | 现货 | |
200 mg | ¥ 4,190 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 437 | 现货 |
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. |
靶点活性 | CK1ε:32 nM, CKIδ:711 nM |
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]. |
分子量 | 359.81 |
分子式 | C17H18ClN5O2 |
CAS No. | 1188296-52-7 |
Smiles | Nc1ncnc2n(nc(COc3cccc(Cl)c3)c12)C1CCOCC1 |
密度 | 1.52 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 60 mg/mL (166.76 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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