RU.521

SKU: orb1301750

Description

RU.521

Research Area

Immunology & Inflammation, Molecular Biology

Key Properties

• CAS Number: 2262452-06-0
• MW: 415.23
• Purity: 98.72%
• Formula: C₁₉H₁₂Cl₂N₄O₃
• SMILES: Cc1nn(c(O)c1C1OC(=O)c2ccccc12)-c1nc2ccc(Cl)c(Cl)c2[nH]1
• Target: cGAS,DNA
• Solubility: DMSO:126.3 mg/mL (304.17 mM);5% DMSO+40% PEG300+5% Tween 80+50% Saline:2 mg/mL (4.82 mM)

Bioactivity

• Target IC50:
  THP-1-Dual cells:38.4 μM (CC50)|dsDNA:700 nM|H69AR cells:32.9 μM
• In Vivo:
  METHODS: To study the effect of RU.521 on sepsis, mice were intraperitoneally injected with RU.521 (5 mg/kg) (injected with LPS) in a single dose. RESULTS: RU.521 enhanced cardiac function, reduced cardiac inflammation, oxidative stress and apoptosis, and alleviated the symptoms of sepsis in mice.
• In Vitro:
  METHODS: Human THP1-Dual cells were treated with RU.521 for 24 hours, and the cytotoxicity was determined using the CCK-8 assay. RESULTS: RU.521 inhibited cell growth (CC50=38.4 μM).
• 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.

Storage & Handling

• Storage: keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RU 320521, RU320521, RU-320521, RU.521, oxidative stress, signaling pathway, cGAS, dsDNA/cGAS, Cyclic GMP-AMP Synthase, inflammatory, inhibit, Inhibitor

Compound Identifiers

PubChem CID

135397653