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IT1t抑制剂
发布时间:2017-12-07        浏览次数:53        返回列表
IT1t是高效的<b>CXCR4</b>拮抗剂;抑制CXCL12/CXCR4相互作用的<b>IC<sub>50</sub></b>值为2.1 nM。<BR><a href="https://www.medchemexpress.cn/BAY1125976.html">BAY1125976</a>产品描述:BAY1125976 is a selective allosteric <b> Akt1/2</b> inhibitor; inhibits Akt1 and Akt2 activity with <b>IC<sub>50</sub></b> values of 5.2 nM and 18 nM at 10 μM ATP, respectively.


IC50 & Target: IC50: 5.2 nM (Akt1, at 10 μM ATP), 18 nM (Akt2, at 10 μM ATP)<sup>[1]</sup>
<i><b>In Vitro:</b></i> BAY 1125976 is equally potent against Akt1 (IC<sub>50</sub>=5.2 nM at 10 μM ATP and 44 nM at 2 mM ATP)and Akt2(IC<sub>50</sub>=18 nM at 10 μM ATP and 36 nM at 2 mM ATP) isoforms and up to 86 fold less potent against Akt3 (IC<sub>50</sub>=427 nM at 10 μM ATP). It inhibits the Akt1 and Akt2 by binding into an allosteric binding pocket formed by kinase and PH domain. It inhibits cell proliferation in a broad panel of human cancer cell lines, particularly in breast and prostate cancer cell lines expressing estrogen or androgen receptors. It effectively blocks Akt signaling by inhibiting the phosphorylation of Akt and the downstream effectors, including eukaryotic translation initiation factor 4E b<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);">公司介绍:MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库,总部位于美国新泽西,分别在瑞典和上海设有欧洲区子公司和亚洲区总代理,营销网点遍及全球20多个国家地区。MCE经过多年努力已成为全球生物活性小分子领域的一流供应商, 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域,PI3K、MAPK等近千个细分靶点,超过4000个活性小分子化合物现货,以及GPCR、API、离子通道等超过20种不同类型的化合物库,同时提供从毫克到千克的专业定制合成服务。</span>
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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);">MCE 对每批产品都进行严格的LCMS和NMR检验,其产品已被全球近万名客户广泛使用并发表大量文章、专利;</span>
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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/BAY1125976.html">www.medchemexpress.cn/BAY1125976.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="">Purity:98%<BR>MWt:406.6515<BR>Formula:C21H34N4S2<BR>SMILES:CC1(C)CN2C(CS/C(NC3CCCCC3)=N\C4CCCCC4)=CSC2=N1<BR>Pathway:GPCR/G Protein; Immunology/Inflammation; <BR>Mechanisms:CXCR; <BR>Research Area:Inflammation/Immunology<BR>电话: 021-58955995<BR>网址: www.MedChemExpress.cn <BR>地址: 上海市浦东新区蔡伦路720号2号楼3层