RU.521

Name: RU.521
Brand: Tocris Bioscience
SKU: 7904

Tocris Bioscience, part of Bio-Techne | Catalog # 7904

COA / SDS

Potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS)

Key Product Details

Description:	Potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS)
Alternative Names:	RU320521
Chemical Name:	3-[1-(6,7-Dichloro-1H-benzimidazol-2-yl)-5-hydroxy-3-methyl-1H-pyrazol-4-yl]-1(3H)-isobenzofuranone
Purity:	≥98% (HPLC)
Molecular Weight:	415.23

View Full Technical Details for RU.521

Technical Data
Citations

Biological Activity for RU.521

RU.521 is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor (K_d = 36.2 nM; IC₅₀ values are 0.11 μM and 2.94 μM against m-cGAS and h-cGAS, respectively). RU.521 suppresses dsDNA-activated reporter activity but not 5'ppp-HP20 RNA or murine IFN-β-induced IFN-β1-dependent gene expression. RU.521 reduces constitutive expression of type I interferon in primary macrophages from a mouse model of Aicardi-Goutières syndrome. Pretreatment of chimeric antigen receptor (CAR) redirected T cells with RU.521 increases efficiency of virus-free gene editing by improving cell viability and CAR integration in cell line.

Technical Data for RU.521

M. Wt	415.23
Formula	C₁₉H₁₂Cl₂N₄O₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2262452-06-0
InChi Key	VIQXILLOJLATEF-UHFFFAOYSA-N
Smiles	O=C1OC(C=2C=CC=CC12)C3=C(O)N(N=C3C)C4=NC=5C=CC(Cl)=C(Cl)C5N4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for RU.521

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	20.76	50

Preparing Stock Solutions for RU.521

The following data is based on the product molecular weight 415.23.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	4.82 mL	24.08 mL	48.17 mL
2.5 mM	0.96 mL	4.82 mL	9.63 mL
5 mM	0.48 mL	2.41 mL	4.82 mL
25 mM	0.10 mL	0.48 mL	0.96 mL

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References for RU.521

References are publications that support the biological activity of the product.

Apel The cytosolic DNA sensor cGAS recognizes neutrophil extracellular traps Sci.Signal 2021 PMID: 33688080
Ke cGAS-STING signaling pathway in gastrointestinal inflammatory disease and cancers. FASEB J 2022 PMID: 34907606
Zhou Structure of the Human cGAS-DNA Complex Reveals Enhanced Control of Immune Surveillance. Cell 2018 PMID: 30007416
Vincent Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat.Commun 2017 PMID: 28963528
Lama Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression. Nat.Commun 2019 PMID: 31113940
Kath Pharmacological interventions enhance virus-free generation of TRAC-replaced CAR T cells. Mol.Ther.Methods Clin.Dev 2022 PMID: 35573047