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      CCT251236研究進(jìn)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/CCT251236.htmlCCT251236/a產(chǎn)品描述:CCT251236 is an orally available pirin ligand f
      <a href="https://www.medchemexpress.com/CCT251236.html">CCT251236</a>產(chǎn)品描述:CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an <b>IC<sub>50</sub></b> of 19 nM for inhibition of HSF1-mediated <b>HSP72</b> induction.

      IC50 & Target: IC50: 19 nM (HSF1-mediated HSP72 induction)<sup>[1]</sup>

      <i><b>In Vitro:</b></i> CCT251236 displays the desired balance of <i>in vitro</i> properties, while maintaining excellent cellular activity with an IC<sub>50</sub> of 19 nM. The free GI<sub>50</sub> in SK-OV-3 cells is 1.1 nM. Western blotting confirms that CCT251236 blocks the HSF1-mediated induction of both HSP72 and HSP27 as representative heat shock proteins, following treatment with the HSP90 inhibitor 17AAG. Also, qPCR analysis demonstrates that CCT251236 inhibits the induction of HSP72 at the mRNA level, clearly blocking the induction of HSPA1A gene expression with an IC<sub>50</sub> of 40 nM<sup>[1]</sup>.



      <i><b>In Vivo:</b></i> CCT251236 possesses low total blood clearance (10% hepatic blood fl<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(dòng)劑、API及化合物庫(kù),總部位于美國(guó)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(yíng)銷網(wǎng)點(diǎn)遍及全球20多個(gè)國(guó)家地區(qū)。MCE經(jīng)過(guò)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(gè)熱門研究領(lǐng)域,PI3K、MAPK等近千個(gè)細(xì)分靶點(diǎn),超過(guò)4000個(gè)活性小分子化合物現(xiàn)貨,以及GPCR、API、離子通道等超過(guò)20種不同類型的化合物庫(kù),同時(shí)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(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/cct251236.html">www.medchemexpress.cn/cct251236.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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