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IPI549

发布日期：2017-10-26   浏览次数：0
核心提示：a href=https://www.medchemexpress.com/IPI549.htmlIPI549/a产品描述：IPI549 is a potent and selective bPI3K/b Inhibitor wi
<a href="https://www.medchemexpress.com/IPI549.html">IPI549</a>产品描述：IPI549 is a potent and selective <b>PI3Kγ</b> Inhibitor with <b>IC<sub>50</sub></b> of 16 nM.

IC50 & Target: IC50: 16 nM (PI3Kγ), 3.2 μM (PI3Kα), 3.5 μM (PI3Kβ), >8.4 μM (PI3Kδ)<sup>[1]</sup>

<i><b>In Vitro:</b></i> IPI-549 inhibits PI3Kγ with IC<sub>50</sub> of 16 nM, with >100-fold selectivity over other lipid and protein kinases (PI3Kα IC<sub>50</sub>=3.2 μM, PI3Kβ IC<sub>50</sub>=3.5 μM, PI3Kδ IC<sub>50</sub>>8.4 μM). IPI549 is evaluated for activity across all Class I PI3K isoforms. The binding affinity of IPI549 for PI3K-γ is determined by measuring the individual rates constants and for PI3K-α, β and δ using equilibrium fluorescent titration. IPI549 is found to be a remarkably tight binder to PI3Kγ with a K<sub>d</sub> of 290 pM and >58-fold weaker affinity for other Class I PI3K isoforms (PI3Kα K<sub>d</sub>=17 nM, PI3Kβ K<sub>d</sub>=82 nM, PI3Kδ K<sub>d</sub>=23 M). In PI3K-α, -β, -γ, and -δ dependent cellular phospho-AKT assays, IPI549 demonstrates excellent PI3K-γ potenc<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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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/ipi549.html">www.medchemexpress.cn/ipi549.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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