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Submit ReviewCU-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.
分子量 | 407.12 |
公式 | C11H8F2IN5O2 |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 40.71 | 100 | |
ethanol | 4.07 | 10 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for CU-76, please let us know.
关键词: 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
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