BX-912
| CAS号 | 702674-56-4 | 货号 | BCP01898 |
| 中文名 | BX-912 | ||
| 英文名 | BX-912 | ||
| 中文别名 | |||
| 英文别名 | BX912;BX 912; | ||
| 分子式 | C20H23BrN8O | 分子量 | 471.36 |
| 生物活性 | BX912 prevents ChcK1, PKA, c-kit, and KDR with IC50 of 0.83, 0.11, 0.85, and 0.41 μM, resepectively. BX912 blocks PDK1/Akt signaling in tumor cells and suppresses the anchorage-dependent growth of a variety of tumor cell lines (such as PC-3 cells ) in culture or induces apoptosis. A number of cancer cell lines (such as MDA-468 breast cancer) with elevated Akt activity are >30-fold more sensitive to growth inhibition by PDK1 inhibitor BX912 in soft agar than on tissue culture plastic, consistent with the cell survival function of the PDK1/Akt signaling pathway, which is particularly important for unattached cells. BX912 potently blocks PDK1 enzyme activity in a direct kinase assay format, although BX912 fails to block preactivated AKT2 activity (IC50 > 10 μM). Therefore, BX-912 is a direct inhibitor of PDK1. BX912 is a competitive inhibitor of PDK1 activity with respect to its substrate, ATP, suggesting that BX912 binds to the ATP binding pocket of PDK1. The aminopyrimidine backbone of | ||
| 信号通路 | PI3K/Akt/mTOR | ||
| 靶 点 | PDK | ||
结构式
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