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RU.521

Catalog No. T5486   CAS 2262452-06-0
Synonyms: RU320521

RU.521 (RU3205217) is a potent dsDNA inhibitor (IC50 : 700 nM), inhibition of the dsDNA pathway by RU.521 requires the presence of cGAS.

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RU.521 Chemical Structure
RU.521, CAS 2262452-06-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 41.00
2 mg In stock $ 58.00
5 mg In stock $ 97.00
10 mg In stock $ 172.00
25 mg In stock $ 281.00
50 mg In stock $ 396.00
100 mg In stock $ 589.00
1 mL * 10 mM (in DMSO) In stock $ 97.00
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Purity: 99.82%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description RU.521 (RU3205217) is a potent dsDNA inhibitor (IC50 : 700 nM), inhibition of the dsDNA pathway by RU.521 requires the presence of cGAS.
Targets&IC50 dsDNA:700 nM
In vivo 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.
Cell Research 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.
Animal Research 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.
Synonyms RU320521
Molecular Weight 415.23
Formula C19H12Cl2N4O3
CAS No. 2262452-06-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (301.04 mM)

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Immunology/Inflammation Compound Library Bioactive Compound Library DNA Damage & Repair Compound Library

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Keywords

RU.521 2262452-06-0 DNA Damage/DNA Repair Immunology/Inflammation DNA cGAS inflammatory oxidative stress Inhibitor inhibit RU 320521 Cyclic GMP-AMP Synthase RU-320521 RU320521 signaling pathway inhibitor

 

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