|N-(3-(4-氟苯基磺酰氨基)-4-甲氧基苯基)-[1,1'-联苯]-4-甲酰胺|CsnPharm

CAS No.: 727699-84-5

SN-001 Catalog No. CSN29564

Synonyms: N-[3-(4-fluorobenzenesulfonamido)-4-methoxyphenyl]-4-phenylbenzamide

DUN99845 was reported as a STING inhbiitor, which inhibited the activation of the STING signal pathway and to prevent or treat a STING-mediated disease.

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技术信息

生物活性

描述The cGAS-STING signalling axis, comprising the synthase for the second messenger cyclic GMP-AMP (cGAS) and the cyclic GMP-AMP receptor stimulator of interferon genes (STING), detects pathogenic DNA to trigger an innate immune reaction involving a strong type I interferon response against microbial infections^[1]. The cGAS-STING pathway responds to viral, bacterial, and self-DNA. Whereas it generally mediates immune surveillance and is often neuroprotective, excessive engagement of the system can be deleterious^[2]. STING-deficient mice exhibited unaltered initial development of HCC, but had higher number of large tumors at late stages of disease. In the liver of STING-deficient HCC mice, we observed reduced levels of phospho-STAT1, autophagy, and cleaved caspase3. These responses were activated in the liver by treatment with a cyclic dinucleotide (CDN) STING agonist. Importantly, CDN treatment of mice after HCC development efficiently reduced tumor size^[3]. STING and IRF3 were upregulated in livers of HFD-fed mice and in FFA-induced L-O2 cells. Knocking down either STING or IRF3 led to a significant reduction in FFA-induced hepatic inflammation and apoptosis, as evidenced by modulation of the nuclear factor κB (NF-κB) signaling pathway, inflammatory cytokines, and apoptotic signaling. Additionally, STING/IRF3 knockdown enhanced glycogen storage and alleviated lipid accumulation, which were found to be associated with increased expression of hepatic enzymes in glycolysis and lipid catabolism, and attenuated expression of hepatic enzymes in gluconeogenesis and lipid synthesis. GUN35901 is a demethyl analogue of DUN99845. GUN35901 is a STING inhibitor, which inhibited the activation of the STING signal pathway and to prevent or treat a STING- mediated disease^[4].
参考文献

[1] Karl-Peter Hopfner,Veit Hornung. Molecular mechanisms and cellular functions of cGAS-STING signalling. Nat Rev Mol Cell Biol. 2020 Sep;21(9):501-521.
[2] Bindu D Paul,et al. Signaling by cGAS-STING in Neurodegeneration, Neuroinflammation, and Aging. Trends Neurosci. 2021 Feb;44(2):83-96.
[3] Martin K Thomsen,et al. The cGAS-STING pathway is a therapeutic target in a preclinical model of hepatocellular carcinoma. Oncogene. 2020 Feb;39(8):1652-1664.
[4] J T Qiao,et al. Activation of the STING-IRF3 pathway promotes hepatocyte inflammation, apoptosis and induces metabolic disorders in nonalcoholic fatty liver disease. Metabolism. 2018 Apr;81:13-24.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0986 mL
- 10.4928 mL
- 20.9855 mL
- 5 mM
- 0.4197 mL
- 2.0986 mL
- 4.1971 mL
- 10 mM
- 0.2099 mL
- 1.0493 mL
- 2.0986 mL

技术信息

CAS号	727699-84-5	储存条件	粉末 Keep in dark place,Sealed in dry,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C26H21FN2O4S	运输	蓝冰
分子量	476.52	别名	N-[3-(4-fluorobenzenesulfonamido)-4-methoxyphenyl]-4-phenylbenzamide

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