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IT1t研究进展

发布日期：2017-10-30   浏览次数：0
核心提示：a href=https://www.medchemexpress.com/IT1t.htmlIT1t/a产品描述：IT1t is a potent bCXCR4/b antagonist; inhibits CXCL12/CXC
<a href="https://www.medchemexpress.com/IT1t.html">IT1t</a>产品描述：IT1t 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 competitive inhibit<br><br>
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已为全球多个知名企业、院校构建各种定制型化合物库。</span><br><br>产品链接：<a href="http://www.medchemexpress.cn/it1t.html">www.medchemexpress.cn/it1t.html</a><br><br></span><img style="width: 600.0px;height: 310.0px;"

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