BX-912,PDK1 抑制剂

BX-912 (订货以英文为准)

编号:B126138
CAS号:702674-56-4
分子式:C20H23BRN8O
分子量:471.35
货号 品牌 包装 目录价 您的价格 库存 数量 购买
B126138-25mg 阿拉丁 25mg ¥799.90
B126138-5mg 阿拉丁 5mg ¥229.90
B126138-100mg 阿拉丁 100mg ¥2299.90
产品名称 BX-912
中文名称 BX-912,PDK1 抑制剂
CAS号 702674-56-4
分子式(M.F.) C20H23BRN8O
分子量(M.W.) 471.35
储存条件 -20°C储存
存贮条件储存温度-20°C
应用A potent and selective PDK-1 inhibitor that induces apoptosis
产品介绍BX-912是一种有效的,特异性的PDK1抑制剂,IC50为12 nM,作用于PKD1比作用于PKA和PKC选择性分别高9和105倍。
备注BX912 is a potent and specific PDK1 inhibitor with IC50 of 12 nM, 9- and 105- fold greater selectivity for PKD1 than PKA and PKC, respectively. In comparison to GSK3β, selectivity for PDK1 is 600-fold.
生化机理BX-912 is a PDK-1 inhibitor. BX 912 suppresses growth in a number of cell lines and also induces apoptosis. Cell lines with elevated levels of AKT are >30-fold more sensitive to PDK1 inhibition by BX-912. This compound is a competitive inhibitor of PDK1, indicating that it binds to the ATP-binding pocket to inhibit phosphorylation. BX-912 accomplishes this due to the fact that the aminopyrimidine backbone, which adopts a similar conformation to ATP in the active site of PDK1. BX-912 potently inhibits the growth of PC-3 cells in soft agar, displaying an IC50 of 320 nM.
别名N-[3-[[5-溴-4-[[2-(1H-咪唑-5-基)乙基]氨基]-2-嘧啶基]氨基]苯基]-1-吡咯烷甲酰胺;BX912;BX 912;N-(3-(4-(2-(1H-imidazol-5-yl)ethylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide
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