CU-76

Pricing Availability   Qty
说明: Selective inhibitor of cyclic GMP-AMP synthase (cGAS)
化学名: Methyl 4-amino-6-[(3,5-difluoro-4-iodophenyl)amino]-1,3,5-triazine-2-carboxylate
纯度: ≥98% (HPLC)
说明书
引用文献
评论

生物活性 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.

技术数据 for CU-76

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.

溶解性数据 for CU-76

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 40.71 100
ethanol 4.07 10

制备储备液 for CU-76

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.

选择批次从而根据批次分子量重新计算:
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

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参考文献 for CU-76

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


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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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