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IT1t (dihydrochloride)研究進(jìn)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/IT1t_dihydrochloride.htmlIT1t (dihydrochloride)/a產(chǎn)品描述：IT1t dihydrochloride is
<a href="https://www.medchemexpress.com/IT1t_dihydrochloride.html">IT1t (dihydrochloride)</a>產(chǎn)品描述：IT1t dihydrochloride is a potent <b>CXCR4</b> antagonist; inhibits CXCL12/CXCR4 interaction with an <b>IC<sub>50</sub></b> of 2.1 nM.

IC50 & Target: IC50: 2.1 nM (CXCL12/CXCR4 interaction)<sup>[1]</sup>

<i><b>In Vitro:</b></i> The CXCR4 is involved in chemotaxis and serves as a coreceptor for T-tropic HIV-1 viral entry and in cancer metastasis. IT1t is a small, drug-like, isothiourea derivative. IT1t shows very potent and dose-dependent inhibition of the CXCL12/CXCR4 interaction with an IC<sub>50</sub> of 2.1 nM. This calcium flux is also inhibited by IT1t with an IC<sub>50</sub> of 23.1<sup>[1]</sup>. Strong electron density is observed for IT1t in the binding cavity of both subunits of the CXCR4 homodimer. In dimers of CXCR4 bound to IT1t, the monomers interact only at the extracellular side of helices V and VI, leaving at least a 4 Å gap between the intracellular regions, which is presumably filled by lipids. The IT1t compound and CVX15 peptide have both been characterized as com<br><br>
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已為全球多個(gè)知名企業(yè)、院校構(gòu)建各種定制型化合物庫(kù)。</span><br><br>產(chǎn)品鏈接：<a href="http://www.medchemexpress.cn/it1t-dihydrochloride.html">www.medchemexpress.cn/it1t-dihydrochloride.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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