AVN-944產(chǎn)品描述:AVN-944(VX-944) is a selective, noncompetitive inhibitor of the enzyme directed against human IMPDH with Ki of 6-10 nM for IMPDH1/IMPDH2.IC50 value: 6-10 nM (Ki) [1]Target: IMPDHin vitro: AVN-944 strikingly inhibit RNA synthesis within 2 h of exposure. Depletion of guanine nucleotides by MPA and AVN-944 also causes an early and near-complete reduction in levels of the 45S precursor rRNA synthesis and the concomitant translocation of nucleolar proteins including nucleolin, nucleophosmin, and nucleostemin from the nucleolus to the nucleoplasm [2]. AVN944 induced caspase-dependentand caspase-independent cell death in LNCaP, CWR22Rv1, and DU145 cells. AVN944 induced expression of p53-target proteins Bok, Bax and Noxa in androgen-responsive cell lines and suppressed expression of survivin in prostate cancer cells regardless of their androgen sensitivity. AVN944 also induced differentiation of androgen-independent prostate cancer cells as indicated by morphological changes and increas 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)品都進行嚴格的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/avn-944.html |
AVN-944研究進展
發(fā)布日期:2017-11-06 瀏覽次數(shù):0
核心提示:a href=https://www.medchemexpress.com/AVN-944.htmlAVN-944/a產(chǎn)品描述:AVN-944(VX-944) is a selective, noncompetitive inhi
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