CU-76

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Description: Selective inhibitor of cyclic GMP-AMP synthase (cGAS)
Chemical Name: Methyl 4-amino-6-[(3,5-difluoro-4-iodophenyl)amino]-1,3,5-triazine-2-carboxylate
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews

Biological Activity for CU-76

CU-76 is a selective cyclic GMP-AMP synthase (cGAS) inhibitor (IC50 = 0.24 μM). It specifically inhibits cGAS-STING pathway and has no effect on other nucleic acid sensing pathways such as the RIG-I-MAVS or Toll-like receptor pathways. CU-76 reduces DNA-induced IFN regulatory factor 3 (IRF3) dimerization in a dose-dependent manner, and it decreases production of IFN-β in THP-1 cells stimulated with interferon-stimulatory DNA.

Technical Data for CU-76

M. Wt 407.12
Formula C11H8F2IN5O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2400954-58-5
PubChem ID 156588964
InChI Key DATILFYUDSRBBK-UHFFFAOYSA-N
Smiles O=C(C1=NC(NC2=CC(F)=C(C(F)=C2)I)=NC(N)=N1)OC

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 CU-76

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 40.71 100
ethanol 4.07 10

Preparing Stock Solutions for CU-76

The following data is based on the product molecular weight 407.12. 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
1 mM 2.46 mL 12.28 mL 24.56 mL
5 mM 0.49 mL 2.46 mL 4.91 mL
10 mM 0.25 mL 1.23 mL 2.46 mL
50 mM 0.05 mL 0.25 mL 0.49 mL

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References for CU-76

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

Salinas et al (2020) Discovery of small-molecule cyclic GMP-AMP synthase inhibitors. J.Org.Chem 85 1579 PMID: 31829590

Li et al (2021) Therapeutic development by targeting the cGAS-STING pathway in autoimmune disease and cancer. Front Pharmacol 12 779425 PMID: 34867409

Wang et al (2021) Small molecule approaches to treat autoimmune and inflammatory diseases (Part II): Nucleic acid sensing antagonists and inhibitors. Bioorg.Med.Chem.Lett 44 128101 PMID: 33984476


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Keywords: CU-76, CU-76 supplier, CU76, selective, inhibitor, inhibits, cyclic, GMP-AMP, synthase, cGAS, cytosolic, DNA, sensing, cGAS-STING, STING, GMP, AMP, STING-Dependent, Signaling, Cytokines, 7820, Tocris Bioscience

Citations for CU-76

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