RU.521

Synonyms: RU320521

RU.521 (RU320521) is an active, potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS) that inhibits the cGAS-mediated signaling with IC50 of 700 nM. RU.521 binds to the cGAS/dsDNA complex with Kd of 36.2 nM.

RU.521 Chemical Structure

RU.521 Chemical Structure

CAS No. 2262452-06-0

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RU.521 Related Products

Biological Activity

Description RU.521 (RU320521) is an active, potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS) that inhibits the cGAS-mediated signaling with IC50 of 700 nM. RU.521 binds to the cGAS/dsDNA complex with Kd of 36.2 nM.
Targets
cGAS/dsDNA complex [1]
(Cell-free assay)
cGAS [1]
(Cell-free assay)
36.2 nM(Kd) 700 nM
In vitro
In vitro

RU.521, a cGAS inhibitor, impares the overexpression of interferon-stimulated genes (ISGs) in response to cytolethal distending toxin (CDT), confirming the crucial role of cGAS-STING axis in CDT-induced type I IFN signaling.[2]

Cell Research Cell lines Mouse Embryonic Fibroblasts (MEFs)
Concentrations 1 μM
Incubation Time 3, 7, 40 days
Method

MEFs are exposed with or without STINGi or cGASi to CDT 7.5 ng/ml for the indicated times or to the H153A CDT mutant for 40 days. The mRNA level of the indicated genes is analyzed by RT-qPCR and the IL-6 or TNFα production in the culture supernatant are determined by ELISA. For ELISA assays, a 2 days exposure to LPS 100 ng/ml is used as positive control.

In Vivo
In vivo

RU.521 alleviated the inflammatory response and alleviated the damage induced by oxidative stress, leading to cardiac protection via increased Sirt3 expression in the hearts of mice with sepsis.

Animal Research Animal Models Mice
Dosages 5 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 415.23 Formula

C19H12Cl2N4O3

CAS No. 2262452-06-0 SDF --
Smiles CC1=C(C(=O)N(N1)C2=NC3=C(N2)C=CC(=C3Cl)Cl)C4C5=CC=CC=C5C(=O)O4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 83 mg/mL ( (199.88 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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