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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>
      
            <br>
      
            <span style="outline: 0.0px;line-height: 22.0px;color:   rgb(62,62,62);font-family: "Helvetica Neue" , Helvetica , Arial ,   sans-serif;font-size: 11.818182px;background-color:   rgb(251,251,251);">公司介紹：MedChemExpress(MCE)專注于各種抑制劑、激動劑、API及化合物庫，總部位于美國新澤西，分別在瑞典和上海設(shè)有歐洲區(qū)子公司和亞洲區(qū)總代理，營銷網(wǎng)點遍及全球20多個國家地區(qū)。MCE經(jīng)過多年努力已成為全球生物活性小分子領(lǐng)域的一流供應(yīng)商，   產(chǎn)品涵蓋癌癥、神經(jīng)科學(xué)、抗感染、表觀遺傳學(xué)等20個熱門研究領(lǐng)域，PI3K、MAPK等近千個細分靶點，超過4000個活性小分子化合物現(xiàn)貨，以及GPCR、API、離子通道等超過20種不同類型的化合物庫，同時提供從毫克到千克的專業(yè)定制合成服務(wù)。</span>
      
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            已為全球多個知名企業(yè)、院校構(gòu)建各種定制型化合物庫。</span><br><br>產(chǎn)品鏈接：<a   href="http://www.medchemexpress.cn/hi-topk-032.html">www.medchemexpress.cn/hi-topk-032.html</a><br><br></span><img   style="width: 600.0px;height: 310.0px;" 
      
            
      
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