PF-3758309產(chǎn)品描述:PF-3758309 is an inhbitor of PAK with IC50 of 1.3 nM for PAK4.IC50 & Target: IC50: 1.3 nM (PAK4)In Vitro: F-3758309 binds directly to PAK4 with an in vitro potency of 2.7-4.5 nM. PF-3758309 has similar enzymatic potency against the kinase domains of the other group B PAKs (PAK5, Ki=18.1±5.1 nM; PAK6, Ki=17.1±5.3 nM) and group A PAK1 (Ki=13.7±1.8 nM), but is less active against the other two group A PAKs (PAK2, IC50=190 nM; PAK3, IC50=99 nM). PAK4 phosphorylates GEF-H1 on a previously characterized serine residue 810 and is inhibited by PF-3758309 (IC50=1.3±0.5 nM). PF-3758309 also inhibits endogenous pGEF-H1 accumulation in HCT116 cells[1]. PF-3758309 is profiled for its growth-inhibitory activity in a panel of 92 tumor cell lines, half of which exhibits IC50 values of less than 10 nM[2]. The proliferation of A549 cells is affected at the treatm 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(shè)有歐洲區(qū)子公司和亞洲區(qū)總代理,營銷網(wǎng)點遍及全球20多個國家地區(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個熱門研究領(lǐng)域,PI3K、MAPK等近千個細(xì)分靶點,超過4000個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,同時提供從毫克到千克的專業(yè)定制合成服務(wù)。 MCE 對每批產(chǎn)品都進(jìn)行嚴(yán)格的LCMS和NMR檢驗,其產(chǎn)品已被全球近萬名客戶廣泛使用并發(fā)表大量文章、專利; MCE 定期增加各領(lǐng)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; 數(shù)千種產(chǎn)品在上海有充足備貨,24-48小時內(nèi)送達(dá)客戶; 大量產(chǎn)品提供免費試用裝;已為全球多個知名企業(yè)、院校構(gòu)建各種定制型化合物庫。 產(chǎn)品鏈接:www.medchemexpress.cn/pf-3758309.html |
PF-3758309研究進(jìn)展
發(fā)布日期:2017-11-01 瀏覽次數(shù):2
核心提示:a href=https://www.medchemexpress.com/PF-3758309.htmlPF-3758309/a產(chǎn)品描述:PF-3758309 is an inhbitor of bPAK/b with bICs
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