HI-TOPK-032
| CAS号 | 487020-03-1 | 货号 | BCP35692 |
| 中文名 | HI-TOPK-032 | ||
| 英文名 | HI-TOPK-032 | ||
| 中文别名 | |||
| 英文别名 | HI-TOPK032; HI-TOPK 032; | ||
| 分子式 | C20H11N5OS | 分子量 | 369.4 |
| 生物活性 | HI-TOPK-032 is a potent and selective TOPK inhibitor. In vitro, HI-TOPK-032 strongly suppressed TOPK kinase activity but had little effect on extracellular signal–regulated kinase 1 (ERK1), c-jun—NH2—kinase 1, or p38 kinase activities. HI-TOPK-032 also inhibited anchorage-dependent and -independent colon cancer cell growth by reducing ERK-RSK phosphorylation as well as increasing colon cancer cell apoptosis through regulation of the abundance of p53, cleaved caspase-7, and cleaved PARP. In vivo, administration of HI-TOPK-032 suppressed tumor growth in a colon cancer xenograft model. HI-TOPK-032 may be further developed as a potential therapeutic against colorectal cancer. The serine-threonine mitogen-activated protein kinase kinase family member T-LAK cell–originated protein kinase (TOPK/PBK) is heavily involved in tumor development, cancer growth, apoptosis, and inflammation ( Cancer Res; 72(12); 3060–8.). | ||
| 信号通路 | MAPK Pathway | ||
| 靶 点 | TOPK | ||
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PBK/TOPK Inhibitor Suppresses the Progression of Prolactinomas
购于瀚香生物(Biochempartner)的HI-TOPK-032(CAS:487020-03-1)被引用 |
结构式
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