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GDC-0152研究進展

發(fā)布日期:2017-11-06   瀏覽次數:0
核心提示:a href=https://www.medchemexpress.com/GDC-0152.htmlGDC-0152/a產品描述: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,營銷網點遍及全球20多個國家地區(qū)。MCE經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><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 對每批產品都進行嚴格的LCMS和NMR檢驗,其產品已被全球近萬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 定期增加各領域熱門抑制劑、激動劑,不斷擴增已有化合物庫,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);">數千種產品在上海有充足備貨,24-48小時內送達客戶;</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);">大量產品提供免費試用裝;</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/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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