| 产品描述： | RU.521 (RU320521) is a potent dsDNA inhibitor (IC50 : 700 nM), inhibition of the dsDNA pathway by RU.521 requires the presence of cGAS. |
| 靶点： |
DNA; cGAS;DNA; cGAS |
| 体内研究： |
Treatment of primary BMDMs with RU.521 or its analogs reduced IFNB1 expression in mice, indicating their effectiveness in suppressing intrinsic DNA-dependent, constitutively-activated type I interferon expression in cells deficient of a cytoplasmic DNA exonuclease. |
| 细胞实验： |
Small-molecule compounds were serially diluted to concentrations spanning the range tested in the response curves were added to 6.7 × 10^5 RAW-Blue macrophages plated 16h prior in 96-well dishes, then harvested 72h after compound addition. ATP was measured using CellTiter Glo Viability Assay using 50 μM Tamoxifen as a positive control for cytotoxicity. Viability values were generated using vehicle (DMSO) or the first dose as 100% and Tamoxifen as 0%. Outliers were removed. |
| 动物实验： |
the chronically elevated levels of cytokines observed in Trex1 null mice are a consequence of constitutively activated cGAS, due to the inability to eliminate aberrantly localized self-DNA. We harvested BMDMs from 6–8-week old Trex1 -/- mice, treated them with each compound, and measured expression levels of IFNB1 by quantitative reverse transcription PCR (qRT-PCR). Treatment of primary BMDMs with RU.521 or its analogs reduced IFNB1 expression, indicating their effectiveness in suppressing intrinsic DNA-dependent, constitutively-activated type I interferon expression in cells deficient of a cytoplasmic DNA exonuclease. |
| 参考文献： |
1. Vincent J, et al. Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat Commun. 2017 Sep 29;8(1):750. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.408 ml |
12.042 ml |
24.083 ml |
| 5 mM |
0.482 ml |
2.408 ml |
4.817 ml |
| 10 mM |
0.241 ml |
1.204 ml |
2.408 ml |
| 50 mM |
0.048 ml |
0.241 ml |
0.482 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京