2024548-03-4
2024548-03-4 結(jié)構(gòu)式
基本信息
4-(7-(4-((苯甲氧基)羰基)哌嗪-1-基)-4,4-二甲基-8-硝基苯并吡喃并[4,3-C]吡唑-1(4H)-基)苯甲酸
Lin28-let-7a antagonist 1
Inhibitor,inhibit,MicroRNA,Lin-28-let-7a antagonist 1,Lin28 let 7a antagonist 1,miRNA,Lin28let7a antagonist 1
4-(7-(4-((Benzyloxy)carbonyl)piperazin-1-yl)-4,4-dimethyl-8-nitrochromeno[4,3-c]pyrazol-1(4H)-yl)benzoic acid
1-Piperazinecarboxylic acid, 4-[1-(4-carboxyphenyl)-1,4-dihydro-4,4-dimethyl-8-nitro[1]benzopyrano[4,3-c]pyrazol-7-yl]-, 1-(phenylmethyl) ester
物理化學(xué)性質(zhì)
常見問題列表
IC50：4.03 μM (Lin28A-let-7a-1).
Lin28-let-7a antagonist 1 (compound 1) shows a clear antagonistic effect against the Lin28A-let-7a-1 interaction with an IC 50 of 4.03 μM. Interestingly, Lin28-let-7a antagonist 1 also inhibits the Lin28B-let-7 interaction, with slightly reduced potency. Dicer processing assay reveals that Lin28-let-7a antagonist 1 clearly blocks the formation of the Lin28A-pre-let-7g complex and induces miRNA processing, resulting in the generation of mature let-7g miRNA. When the expression of both Lin28A and Lin28B are knocked-down using siRNA in JAR cells, the Lin28-let-7a antagonist 1-induced increase in cellular let-7 levels is clearly attenuated. Lin28A-let-7a-IN-1 increases mature let-7 levels in PA-1 cells that express high level of Lin28A. On the other hand, let-7 levels are not affected by 1 in MCF7 cells that rarely express Lin28 proteins. Taken together, Lin28-let-7a antagonist 1 specifically induces the increase in the cellular let-7 levels by targeting Lin28.