SML2934
VZ185
≥98% (HPLC)
别名:
(2S,4R)-N-(2-(5-(4-(2,6-Dimethoxy-4-(2-methyl-1-oxo-1,2-dihydro-2,7-naphthyridin-4-yl)benzyl)piperazin-1-yl)pentyloxy)-4-(4-methylthiazol-5-yl)benzyl)-1-((S)-2-(1-fluorocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide, VZ 185, VZ-185
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About This Item
生化/生理作用
VZ185 is a potent and selective bromodomain proteins BRD7 and BRD9 degrader that targets BRD7/9 for von Hippel-Lindau (VHL) ubiquitin ligase complex-mediated degradation. VZ185 effectively induces cellular BRD7/9 degradation (by 90% BRD7 & 86% BRD9 in 4 h in HeLa cells, by 84% BRD7 in 2 h in RI-1 cells; BRD7/9 IC50 = 4.5/1.76 nM in 8 h in RI-1 cells) and exerts potent cytotoxicity in BRD9-dependent cancer cultures (IC50 = 3.389 nM/EOL-1 & 39.81 nM/A-204 post 7-day treatment).
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Vittoria Zoppi et al.
Journal of medicinal chemistry, 62(2), 699-726 (2018-12-13)
Developing PROTACs to redirect the ubiquitination activity of E3 ligases and potently degrade a target protein within cells can be a lengthy and unpredictable process, and it remains unclear whether any combination of E3 and target might be productive for
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