产品描述
| 溶解性 |
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| 存贮条件 | 储存温度-20°C |
| 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 |
