Product Details
| Product Name:
RU.521 |
CAS No.:
2262452-06-0 |
| Purity:
99.82% |
Supply Ability:
10g |
| Release date:
2025/11/05 |
Product Introduction
Bioactivity
| Name | RU.521 |
| Description | RU.521 (RU3205217) is a selective cyclic GMP-AMP synthetase (cGAS) inhibitor (mouse: IC50=0.11 μM), (human: IC50=2.94 μM). RU.521 is an inhibitor of the receptor activated by dsDNA (IC50=700 nM). RU.521 inhibits cGAS-mediated interferon upregulation. RU.521 reduces constitutive interferon expression in macrophages derived from a mouse model of Aicardi-Goutieres syndrome. |
| 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. |
| 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). [1] |
| 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. [2] |
| 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. |
| Solubility Information | 5% DMSO+40% PEG300+5% Tween 80+50% Saline : 2 mg/mL (4.82 mM)
DMSO : 126.3 mg/mL (304.17 mM), Sonication is recommended.
|
| Keywords | signaling pathway | RU-320521 | RU.521 | RU 320521 | oxidative stress | Inhibitor | inhibit | inflammatory | dsDNA/cGAS | Cyclic GMP-AMP Synthase | cGAS |
| Inhibitors Related | Norharmane | Cyclophosphamide hydrate | AOH1996 | Quinacrine dihydrochloride | Elinafide | Clofazimine | L82 | Proflavine Hemisulfate | Hydroxychloroquine sulfate | Methoxsalen | Cyclophosphamide | Crystal Violet |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Bioactive Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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