NVP 231產(chǎn)品描述:NVP-231 is a potent, specific, and reversible CerK inhibitor(IC50=12±2 nM) that competitively inhibits binding of ceramide to CerK.IC50 Value: 12±2 nM [1]Target: CERKin vitro: NVP-231 showed an IC50 value of 12 ± 2 nM and 90% inhibition at 100 nM in the radioassay. NVP-231 did not compete with ATP but rather with ceramide, displaying an inhibition constant (Ki) of 7.4 nM. Furthermore, inhibition by NVP-231 was instantaneous and fully reversible, implying that this compound does not covalently modify CerK. At 10 nM, NVP-231 inhibited C1P formation by >50%; at 100 nM, NVP-231 achieved complete inhibition. Thus the potency and efficacy of NVP-231 observed in cell culture are consistent with those found in vitro. It is noteworthy that, NVP-231 did not inhibit GlcCer and SM formation; rather, it increased these metabolites in correlation with compound concentration, demonstrating that NVP-231 does not act as a general inhibitor of ceramide metabolism [1]. The EC(50) of NVP-231 in thi 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)。 MCE 對(duì)每批產(chǎn)品都進(jìn)行嚴(yán)格的LCMS和NMR檢驗(yàn),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(dòng)劑,不斷擴(kuò)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(shí)內(nèi)送達(dá)客戶; 大量產(chǎn)品提供免費(fèi)試用裝;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。 產(chǎn)品鏈接:www.medchemexpress.cn/nvp-231.html |
NVP 231研究進(jìn)展
發(fā)布日期:2017-11-02 瀏覽次數(shù):0
核心提示:a href=https://www.medchemexpress.com/NVP-231.htmlNVP 231/a產(chǎn)品描述:NVP-231 is a potent, specific, and reversible CerK
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