中文名 | PRT4165 |
英文名 | PRT4165 |
别名 | PRT4165游离态 化合物PRT 4165 H2A泛素化抑制剂(PRT4165) 2-(3-吡啶亚甲基)-1,3-茚满二酮 |
英文别名 | PRT4165 PRT 4165 PRT-4165 NSC 600157 NSC600157 NSC-600157 NSC 600157 PRT 4165(NSC 600157) 2-(3-Pyridylmethylene)-1,3-indandione 2-(pyridin-3-ylmethylidene)indene-1,3-dione 2-(3-Pyridinylmethylene)-1H-indene-1,3(2H)-dione 1H-Indene-1,3(2H)-dione, 2-(3-pyridinylmethylene)- |
CAS | 31083-55-3 |
化学式 | C15H9NO2 |
分子量 | 235.24 |
密度 | 1.1757 (rough estimate) |
沸点 | 377.63°C (rough estimate) |
溶解度 | DMSO: 可溶20mg/mL,澄清 |
折射率 | 1.6231 (estimate) |
存储条件 | 2-8°C |
稳定性 | 从提供的购买之日起稳定1年。DMSO或乙醇中的溶液可以在-20 °C下储存长达3个月。 |
外观 | 粉末 |
颜色 | white to beige |
体外研究 | PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation. In vitro E3 ubiquitin ligase activity assays reveal that PRT4165 inhibits both RNF2 and RING 1A, but not RNF8 nor RNF168. In the presence of PRT4165, H2A ubiquitylation can be completely inhibited regardless of whether RING1 or RNF2 contributes the E3 ubiquitin ligase activity. Treatment of cells for 60 min with 50 μM PRT4165 results in a dramatic reduction in total ubiquitylated histone H2A. It is also found that longer exposure of the cells with the PRT4165 (30 and 60 min) leads to increased levels of γ-H2AX in unirradiated cells. PRT4165 inhibits double-strand break (DSB) repair at the 8-h time point compare with mock treated cells. Cells treated with increasing concentrations of PRT4165 show increasing numbers of cells in G 2 /M. |
WGK Germany | 3 |
RTECS | NK6710000 |
上游原料 | 1,3-茚满二酮 3-吡啶甲醛 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.251 ml | 21.255 ml | 42.51 ml |
5 mM | 0.85 ml | 4.251 ml | 8.502 ml |
10 mM | 0.425 ml | 2.126 ml | 4.251 ml |
5 mM | 0.085 ml | 0.425 ml | 0.85 ml |
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