耗材描述

• 分子式 C₁₆H₁₃BrF₃IN₂O₄
• 分子量561.1
• Beilstein号
• EC号
• MDL号
• PubChem编号

属性

溶解性	DMSO 112 mg/mL Water <1 mg/mL Ethanol 14 mg/mL
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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