名称 | RU.521 |
描述 | RU.521 (RU3205217) is a potent dsDNA inhibitor (IC50 : 700 nM), inhibition of the dsDNA pathway by RU.521 requires the presence of cGAS. |
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 16?h prior in 96-well dishes, then harvested 72?h 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. |
体内活性 | 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. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 125 mg/mL (301.04 mM)
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关键字 | inflammatory | oxidative stress | RU.521 | cGAS | Inhibitor | inhibit | RU 320521 | Cyclic GMP-AMP Synthase | RU-320521 | signaling pathway |
相关产品 | Norharmane | Cyclophosphamide hydrate | Quinacrine dihydrochloride | L82 | Proflavine Hemisulfate | Chromium picolinate | Clofazimine | Hydroxychloroquine sulfate | Methoxsalen | Tallimustine HCl | Cyclophosphamide | Crystal Violet |
相关库 | DNA 损伤和修复分子库 | 经典已知活性库 | 抑制剂库 | NO PAINS 化合物库 | 抗衰老化合物库 | 已知活性化合物库 |