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IT1t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/IT1t.htmlIT1t/a產品描述：IT1t is a potent bCXCR4/b antagonist; inhibits CXCL12/CXC
<a href="https://www.medchemexpress.com/IT1t.html">IT1t</a>產品描述：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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<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域的一流供應商， 產品涵蓋癌癥、神經(jīng)科學、抗感染、表觀遺傳學等20個熱門研究領域，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。</span>
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已為全球多個知名企業(yè)、院校構建各種定制型化合物庫。</span><br><br>產品鏈接：<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;"

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

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