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PD318088
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
阿拉丁 | 生产商 | 上海 | 现货 |
产品参数
货号 | CAS号 | 操作 |
---|---|---|
P125156-100mg | 391210-00-7 | 询价 |
P125156-1mg | 391210-00-7 | 询价 |
P125156-25mg | 391210-00-7 | 询价 |
P125156-5mg | 391210-00-7 | 询价 |
产品介绍
属性
溶解性 |
|
存贮条件 | 储存温度-20°C |
描述
应用 | A small molecule inhibitor of MEK-1 and MEK-2 |
产品介绍 | PD318088是ATP非竞争性MEK1/2变构抑制剂,能与ATP同时结合于MEK1,且其结合位点与ATP结合位点相邻。 |
生化机理 | PD318088 is a small-molecule inhibitor of MEK1/2, which is an analog of PD184352, suggesting it might have substantial anti-proliferative activity against cancer cells, although no functional study of PD318088 is currently available. PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. Formation of the ternary complexes with PD318088 and MgATP results in moderate increases (to 140 nM) for the Kd monomer-dimer for both MEK1 and MEK2. The binding of PD318088 and MgATP to MEK1 also abolishes the formation of tetramers and higher-order aggregates. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM, suggesting that the mechanism of inhibition for PD318088 is probably a result of localized conformational changes in the active site and not a global change in the overall structure. |
别名 | PD 318088;PD-318088; 5-溴-N-(2,3-二羟基丙氧基)-3,4-二氟-2-[(2-氟-4-碘苯基)氨基]苯甲酰胺;PD 318088;PD-318088;5-Bromo-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]benzamide |
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途