D4476CAS号: 301836-43-1分子式: C23H18N4O3分子量: 398.41描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)
产品描述 | |
描述 |
D4476是一种选择性的酪蛋白激酶1 (CK1)和TGF-β 1受体(ALK5)抑制剂, IC50分别为0.3 µM和0.5 µM,最初是作为ALK5抑制剂。 |
纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
Casein Kinase I Inhibitor
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外观 |
淡黄色固体
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可溶性/溶解性 |
Ethanol :19.9 mg/mL (50 mM)
DMSO :39.8 mg/mL (100 mM) |
生物活性 | |
靶点 |
Casein Kinase
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In vitro(体外研究) |
D4476 is a potent and rather selective inhibitor of CK1 in vitro and in cells. In H4IIE hepatoma cells, D4476 specifically inhibits the phosphorylation of endogenous forkhead box transcription factor O1a (FOXO1a) on Ser322 and Ser325 within its MPD, without affecting the phosphorylation of other sites. CK1δ assayed at 0.1 mM ATP using a phosphorylated peptide TFRPRTSpSNASTIS corresponding to residues 312–325 of FOXO1a is inhibited with an IC50 value of 0.3 μM. The IC50 value for CK1δ decreases progressively as the concentration of ATP is lowered, indicating that D4476 is an ATP-competitive inhibitor of CK1. CK1.
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分子结构图