RU.521
Tocris Bioscience, part of Bio-Techne | Catalog # 7904
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
Product Description
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.Product Specifications
Molecular Weight
415.23
Formula
C19H12Cl2N4O3
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
3-[1-(6,7-Dichloro-1H-benzimidazol-2-yl)-5-hydroxy-3-methyl-1H-pyrazol-4-yl]-1(3H)-isobenzofuranone
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for RU.521
For research use only
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