Poloxin
| CAS号 | 321688-88-4 | 货号 | BCP45204 |
| 中文名 | Poloxin | ||
| 英文名 | Poloxin | ||
| 中文别名 | |||
| 英文别名 | |||
| 分子式 | C18H19NO3 | 分子量 | 297.35 |
| 生物活性 | Poloxin is the first small-molecule inhibitor specifically targeting the function of the Plk1 PBD. Poloxin induces centrosome fragmentation and abnormal spindle and chromosome misalignment, which activate the spindle assembly checkpoint and prolong mitosis. Notably, centrosomal fragmentation induced by Poloxin is partially attributable to dysfunctional Kizuna, a key substrate of Plk1 at centrosomes. Moreover, Poloxin strongly inhibits proliferation of a panel of cancer cells by inducing mitotic arrest, followed by a surge of apoptosis. More important, we report, for the first time to our knowledge, that the PBD inhibitor, Poloxin , significantly suppresses tumor growth of cancer cell lines in xenograft mouse models by lowering the proliferation rate and triggering apoptosis in treated tumor tissues. | ||
| 信号通路 | Cell Cycle/DNA Damage | ||
| 靶 点 | PLK | ||
结构式
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