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HI-TOPK-032研究進展

發(fā)布日期：2017-10-30   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/HI-TOPK-032.htmlHI-TOPK-032/a產(chǎn)品描述：HI-TOPK-032 is a potent and specific bTOPK/
<a href="https://www.medchemexpress.com/HI-TOPK-032.html">HI-TOPK-032</a>產(chǎn)品描述：HI-TOPK-032 is a potent and specific <b>TOPK</b> inhibitor.

<i><b>In Vitro:</b></i> HI-TOPK-032 strongly suppresses TOPK kinase activity but has little effect on extracellular signal-regulated kinase 1 (ERK1), c-jun-NH2-kinase 1, or p38 kinase activities. HI-TOPK-032 occupies the ATP-binding site of TOPK and fits the binding site very well. The compound forms hydrogen bonds with GLY83 and ASP151 and has a hydrophobic interaction with LYS30. However, HI-TOPK-032 at the highest concentration (5 μM) also inhibits MEK1 activity by 40%. HI-TOPK-032 also inhibits 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<sup>[1]</sup>.

<i><b>In Vivo:</b></i> Treatment of mice with 1 or 10 mg/kg of HI-TOPK-032 significantly inhibits HCT-116 tumor growth by more than 60% relative to the vehicle-treated group. Mice are well <br><br>
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