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β-Lapachone研究進(jìn)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/_beta_-Lapachone.html-Lapachone/a產(chǎn)品描述：-Lapachone(ARQ-501; beta-lapachone) is
β-Lapachone產(chǎn)品描述：β-Lapachone(ARQ-501; beta-lapachone) is a naturally occurring quinone obtained from the bark of the lapacho tree (Tabebuia avellanedae) with cancer chemopreventive properties; potent inhibitor of IDO1(IC50=0.44 uM).IC50 value: 0.44 uM (IDO1)Target: IDO1 inhibitor; anticancer agentin vitro: β-Lapachone markedly induced cell death without caspase activation. β-Lapachone increased PI uptake and HMGB-1 release to extracellular space, which are markers of necrotic cell death. Necrostatin-1 (a RIP1 kinase inhibitor) markedly inhibited β-lapachone-induced cell death and HMGB-1 release. In addition, β-lapachone activated poly (ADP-ribosyl) polymerase-1(PARP-1) and promoted AIF release, and DPQ (a PARP-1 specific inhibitor) or AIF siRNA blocked β-lapachone-induced cell death [1]. In H9C2 cells, β-lap-mediated elevation of AMPK activity was retarded when the level of Sirt1 was reduced by transfection of siRNA against Sirt1 [2]. β-lapachone was identified as a submicromolar inhibitor of ID


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