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WT-161研究進展

發(fā)布日期：2017-10-27   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/WT-161.htmlWT-161/a產(chǎn)品描述：WT-161 is a potent and selective bHDAC6/b inhibitor w
<a href="https://www.medchemexpress.com/WT-161.html">WT-161</a>產(chǎn)品描述：WT-161 is a potent and selective <b>HDAC6</b> inhibitor with an <b>IC<sub>50</sub></b> of  0.40 nM.



IC50 & Target: IC50: 0.40 nM (HDAC6), 51.61 nM (HDAC3)<sup>[1]</sup>

<i><b>In Vitro:</b></i> WT161 selectively inhibits HDAC6 and dramatically increases levels of acetylated α-tubulin (Ac-α-tubulin) with little effect on global lysine acetylation. WT161 induces significant toxicity in all multiple myeloma cell lines tested, with IC<sub>50</sub>s between 1.5 and 4.7 µM . WT161 in combination with bortezomib triggers significant accumulation of polyubiquitinated proteins and cell stress, followed by caspase activation and apoptosis. More importantly, this combination treatment is effective in bortezomib-resistant cells and in the presence of bone marrow stromal cells, which have been shown to mediate multiple myeloma cell drug resistance<sup>[1]</sup>.

<i><b>In Vivo:</b></i> WT161 shows toxicity at 100 mg/kg i.p., but WT161 is well tolerated at 50 mg/kg i.p.. Bortezomib combined wit<br><br>
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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/wt-161.html">www.medchemexpress.cn/wt-161.html</a><br><br></span><img style="width: 600.0px;height: 310.0px;"

src="http://img.dxycdn.com/trademd/upload/userfiles/image/2014/08/A1408605159png_small.jpg"

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