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GDC-0152研究進(jìn)展

發(fā)布日期：2017-11-06   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/GDC-0152.htmlGDC-0152/a產(chǎn)品描述：GDC-0152 is a potent inhibitor of bIAPs/b which b
<a href="https://www.medchemexpress.com/GDC-0152.html">GDC-0152</a>產(chǎn)品描述：GDC-0152 is a potent inhibitor of <b>IAPs</b> which binds to the <b>XIAP</b> BIR3 domain, the BIR domain of <b>ML-IAP</b>, and the BIR3 domains of <b>cIAP1</b> and <b>cIAP2</b> with <b>K<sub>i</sub></b> values of 28, 14, 17, and 43 nM, respectively.IC50 & Target: Ki: 28 nM (XIAP BIR3), 14 nM (MLIAP-BIR3), 17 nM (cIAP1-BIR3), 43 nM (cIAP2-BIR3)<i><b>In Vitro:</b></i> GDC-0152 can block protein−protein interactions that involve IAP proteins and pro-apoptotic molecules. Using transiently transfected HEK293T cells, GDC-0152 is shown to disrupt XIAP binding to partially processed caspase-9 and to disrupt the association of ML-IAP, cIAP1, and cIAP2 with Smac. In melanoma SK-MEL28 cells, the endogenous association of ML-IAP and Smac is also effectively abolished by GDC-0152. GDC-0152 leads to a decrease in cell viability in the MDA-MB-231 breast cancer cell line, while having no effect on normal human mammary epithelial cells (HMEC). GDC-0152 is found to activate caspases 3 and 7 in a d<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><br style="color: rgb(62,62,62);font-family: "Helvetica Neue" , Helvetica , Arial , sans-serif;font-size: 11.818182px;line-height: 22.0px;background-color: rgb(251,251,251);"><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);">MCE 對(duì)每批產(chǎn)品都進(jìn)行嚴(yán)格的LCMS和NMR檢驗(yàn)，其產(chǎn)品已被全球近萬(wàn)名客戶廣泛使用并發(fā)表大量文章、專利；</span><br style="color: rgb(62,62,62);font-family: "Helvetica Neue" , Helvetica , Arial , sans-serif;font-size: 11.818182px;line-height: 22.0px;background-color: rgb(251,251,251);"><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);">MCE 定期增加各領(lǐng)域熱門抑制劑、激動(dòng)劑，不斷擴(kuò)增已有化合物庫(kù)，以滿足最新的科研需求；</span><br style="color: rgb(62,62,62);font-family: "Helvetica Neue" , Helvetica , Arial , sans-serif;font-size: 11.818182px;line-height: 22.0px;background-color: rgb(251,251,251);"><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);">數(shù)千種產(chǎn)品在上海有充足備貨，24-48小時(shí)內(nèi)送達(dá)客戶；</span><br style="color: rgb(62,62,62);font-family: "Helvetica Neue" , Helvetica , Arial , sans-serif;font-size: 11.818182px;line-height: 22.0px;background-color: rgb(251,251,251);"><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);">大量產(chǎn)品提供免費(fèi)試用裝；</span><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);">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/gdc-0152.html">www.medchemexpress.cn/gdc-0152.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" alt="">
 
 
 
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