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GSK583

發(fā)布日期：2017-10-26   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/GSK583.htmlGSK583/a產(chǎn)品描述：GSK583 is a highly potent and selective inhibitor of
<a href="https://www.medchemexpress.com/GSK583.html">GSK583</a>產(chǎn)品描述：GSK583 is a highly potent and selective inhibitor of <b>RIP2 Kinase</b>, with <b>IC<sub>50</sub></b> of 5 nM.

IC50 & Target: IC50: 5 nM (RIP2K)<sup>[1]</sup>

<i><b>In Vitro:</b></i> GSK583 (1 μM) exhibits excellent selectivity in a panel of 300 kinases, including p38α and VEGFR2. GSK583 potently and dose dependently inhibits MDP-stimulated tumor necrosis factor-alpha (TNFα) production with an IC<sub>50</sub> of 8 nM. GSK583 demonstrates only a modest reduction in potency when profiled in a similar MDP-induced TNFα production assay in human whole blood (IC<sub>50</sub> = 237 nM) and rat whole blood (IC<sub>50</sub> = 133 nM)<sup>[1]</sup>.

<i><b>In Vivo:</b></i> GSK583 (0.1, 1, and 10 mg/kg, p.o.) inhibits serum KC (the rodent orthologue of IL-8) levels in rats in a dose-dependent manner, with an IC<sub>50</sub> derived from rat blood concentrations of 50 nM (or 20 ng/mL). Similarly, GSK583 inhibits serum KC levels and recruitment of neutrophils into the peritoneal cavity in mice i<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，總部位于美國新澤西，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，營銷網(wǎng)點(diǎn)遍及全球20多個(gè)國家地區(qū)。MCE經(jīng)過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20種不同類型的化合物庫，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。</span><br><br>產(chǎn)品鏈接：<a href="http://www.medchemexpress.cn/gsk583.html">www.medchemexpress.cn/gsk583.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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