Name: RU.521
Brand: Selleck Chemicals
SKU: S6841
Rating: 5 (9 reviews)

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

CAS: 2262452-06-0

Selleck's RU.521 has been cited by 9 publications

Purity & Quality Control

Batch: Purity: 99.99%

99.99

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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.

References

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	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

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
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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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