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BX-912

品牌 厂商性质 产地 货期
阿拉丁 生产商 上海 现货

询价
产品参数
货号 CAS号 操作
B126138-25mg 702674-56-4 询价
B126138-5mg 702674-56-4 询价
B126138-100mg 702674-56-4 询价
产品介绍

  • 分子式 C20H23BrN8O
  • 分子量471.36
  • Beilstein号
  • EC号
  • MDL号
  • PubChem编号

属性

存贮条件 储存温度-20°C

描述

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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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