| 应用 |
An inhibitor of PDK1, TBK1, and IKK&epsilon |
| 产品介绍 |
BX-795是一种有效的，特异性的PDK1抑制剂，IC50为6 nM，作用于PDK1比作用于PKA和PKC选择性分别高140和1600倍。 |
| 备注 |
BX795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. |
| 生化机理 |
BX 795 is shown to be a specific and potent inhibitor of IκB kinase ε (IKKε), phosphoinositide 3-kinase 1 (PDK1), and TANK-binding kinase 1 (TBK1). These protein kinases regulate production of type 1 interferons during certain infections. BX 795 has been suggested in studies to block nuclear translocation, phosphorylation, and transcriptional activity of interferon regulatory factor 3. This in turn blocks the production of interferon-β in macrophages. Further experiments have shown that BX 795 is capable of blocking the autophosphorylation of overexpressed TBK1 and IκKε. |
| 别名 |
N-[3-[[5-碘-4-[[3-[(2-噻吩基羰基)氨基]丙基]氨基]-2-嘧啶基]氨基]苯基]-1-吡咯烷甲酰胺;BX 795;BX-795;N-[3-[[5-Iodo-4-[[3-[(2-Thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide |
