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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)

Biological Activity for RU.521

RU.521 is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor (Kd = 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
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 Data for RU.521

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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 0.1 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.

Kath et al (2022) Pharmacological interventions enhance virus-free generation of TRAC-replaced CAR T cells. Mol.Ther.Methods Clin.Dev 25 311 PMID: 35573047

Lama et al (2019) Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression. Nat.Commun 10 2261 PMID: 31113940

Vincent et al (2017) Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat.Commun 8 750 PMID: 28963528

Zhou et al (2018) Structure of the Human cGAS-DNA Complex Reveals Enhanced Control of Immune Surveillance. Cell 174 300 PMID: 30007416

Ke et al (2022) cGAS-STING signaling pathway in gastrointestinal inflammatory disease and cancers. FASEB J 36 e22029 PMID: 34907606

Apel et al (2021) The cytosolic DNA sensor cGAS recognizes neutrophil extracellular traps Sci.Signal 14 eaax7942 PMID: 33688080

If you know of a relevant reference for RU.521, please let us know.

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Keywords: RU.521, RU.521 supplier, RU521, RU320521, selective, potent, inhibitor, inhibits, cyclic, GMP-AMP, synthase, cGAS, cytosolic, DNA, sensing, cGAS-STING, STING-Dependent, Signaling, Other, Synthases/Synthetases, 7904, Tocris Bioscience

Citations for RU.521

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