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

CAS No.: 2249435-90-1

SN-011 Catalog No. CSN29565

Synonyms: GUN35901

SN-011 is a STING inhibitor, which inhibited the activation of the STING signal pathway and to prevent or treat a STING-mediated disease. SN-011 is a demethyl analogue of DUN99845.

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技术信息

生物活性

描述The cyclic GMP-AMP synthase (cGAS)-stimulator of interferon genes (STING) pathway mediates anti-microbial innate immunity by inducing the production of type I interferons (IFNs) and inflammatory cytokines upon recognition of microbial DNA. Recent studies reveal that self-DNA from tumors and by-products of genomic instability also activates the cGAS-STING pathway and either promotes or inhibits tumor development^[1]. On the one hand, the cGAS-STING axis promotes the clearance of CIN tumors through recruitment of immune cells, thus suppressing tumor progression. On the other hand, the cGAS-STING pathway has been described to be the major regulator in the promotion of metastasis of Chromosomal instability (CIN) tumors^[2]. In renal cells of TFAM KO (knockout) mice, aberrant packaging of the mitochondrial DNA (mtDNA) resulted in its cytosolic translocation, activation of the cytosolic cGAS-stimulator of interferon genes (STING) DNA sensing pathway, and thus cytokine expression and immune cell recruitment^[3]. SN-011 locks STING in an open inactive conformation, which inhibits interferon and inflammatory cytokine induction activated by 2'3'-cGAMP, herpes simplex virus type 1 infection, Trex1 deficiency, overexpression of cGAS-STING, or SAVI STING mutants. In Trex1 -/- mice, SN-011 was well tolerated, strongly inhibited hallmarks of inflammation and autoimmunity disease, and prevented death. Thus, a specific STING inhibitor that binds to the STING CDN-binding pocket is a promising lead compound for STING-driven disease^[4].
参考文献

[1] Li Teng Khoo,Liuh-Yow Chen. Role of the cGAS-STING pathway in cancer development and oncotherapeutic approaches. EMBO Rep. 2018 Dec;19(12):e46935.
[2] Christy Hong,et al. The cGAS Paradox: Contrasting Roles for cGAS-STING Pathway in Chromosomal Instability. Cells. 2019 Oct 10;8(10):1228.
[3] Ki Wung Chung,et al. Mitochondrial Damage and Activation of the STING Pathway Lead to Renal Inflammation and Fibrosis. Cell Metab. 2019 Oct 1;30(4):784-799.e5.
[4] Ze Hong,et al. STING inhibitors target the cyclic dinucleotide binding pocket. Proc Natl Acad Sci U S A. 2021 Jun 15;118(24):e2105465118.

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
- 2.1622 mL
- 10.8110 mL
- 21.6220 mL
- 5 mM
- 0.4324 mL
- 2.1622 mL
- 4.3244 mL
- 10 mM
- 0.2162 mL
- 1.0811 mL
- 2.1622 mL

技术信息

CAS号	2249435-90-1	储存条件	粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C25H19FN2O4S	运输	蓝冰
分子量	462.49	别名	GUN35901

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