SN-011
(Synonyms: N-(3-(4-氟苯基磺酰氨基)-4-羟基苯基)-[1,1'-联苯]-4-甲酰胺) 目录号 : GC49400
A STING antagonist
Cas No.:2249435-90-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
SN-011 is a stimulator of interferon genes (STING) antagonist.1 It binds to the STING cyclic dinucleotide binding site (Kd = 4.03 nM) and inhibits 2’3’-cGAMP-induced Ifnb expression in mouse embryonic fibroblasts (MEFs), mouse bone marrow-derived macrophages (BMDMs), and human foreskin fibroblasts (HFFs; IC50s = 127.5, 107.1, and 502.8 nM, respectively). SN-011 (1 µM) impairs recruitment of IFN regulatory factor 3 (IRF3) or TANK-binding kinase 1 (TBK1) to the STING signalosome in HEK293T cells overexpressing tagged wild-type or SAVI-linked mutant STING and IRF3 or TBK1, as well as inhibits translocation of STING from the endoplasmic reticulum (ER) to the Golgi induced by herpes simplex virus 1 (HSV-1) in HFFs. In vivo, SN-011 (5 mg/kg) increases survival and reduces Ifnb mRNA levels in the Trex1-/- mouse model of Aicardi-GoutiÈres syndrome, an autoimmune disorder characterized by constitutive activation of cGAS and IFN overproduction.
1.Hong, Z., Mei, J., Li, C., et al.STING inhibitors target the cyclic dinucleotide binding pocketProc. Natl. Acad. Sci. USA.118(24)e2105465118(2021)
| Cas No. | 2249435-90-1 | SDF | |
| 别名 | N-(3-(4-氟苯基磺酰氨基)-4-羟基苯基)-[1,1'-联苯]-4-甲酰胺 | ||
| Canonical SMILES | O=C(C1=CC=C(C2=CC=CC=C2)C=C1)NC3=CC=C(C(NS(=O)(C4=CC=C(C=C4)F)=O)=C3)O | ||
| 分子式 | C25H19FN2O4S | 分子量 | 462.5 |
| 溶解度 | DMF: 5 mg/ml,DMSO: 25 mg/ml,Ethanol: 3 mg/ml,PBS (pH 7.2): insol | 储存条件 | -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1622 mL | 10.8108 mL | 21.6216 mL |
| 5 mM | 0.4324 mL | 2.1622 mL | 4.3243 mL |
| 10 mM | 0.2162 mL | 1.0811 mL | 2.1622 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
STING inhibitors target the cyclic dinucleotide binding pocket
Proc Natl Acad Sci U S A 2021 Jun 15;118(24):e2105465118.PMID:34099558DOI:10.1073/pnas.2105465118.
Cytosolic DNA activates cGAS (cytosolic DNA sensor cyclic AMP-GMP synthase)-STING (stimulator of interferon genes) signaling, which triggers interferon and inflammatory responses that help defend against microbial infection and cancer. However, aberrant cytosolic self-DNA in Aicardi-Goutière's syndrome and constituently active gain-of-function mutations in STING in STING-associated vasculopathy with onset in infancy (SAVI) patients lead to excessive type I interferons and proinflammatory cytokines, which cause difficult-to-treat and sometimes fatal autoimmune disease. Here, in silico docking identified a potent STING antagonist SN-011 that binds with higher affinity to the cyclic dinucleotide (CDN)-binding pocket of STING than endogenous 2'3'-cGAMP. 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.
Difference in miRNA expression profiles between two cotton cultivars with distinct salt sensitivity
Mol Biol Rep 2012 Apr;39(4):4961-70.PMID:22160515DOI:10.1007/s11033-011-1292-2.
MicroRNAs (miRNAs) are a class of endogenous, non-coding small RNAs that play important roles in many developmental processes and stress responses in plants and animals. Cotton (Gossypium hirsutum L.) is considered a relatively salt-tolerant non-halophytic plant species. To study the role of miRNAs in salt adaptation, a salt-tolerant cotton cultivar SN-011 and a salt-sensitive cultivar LM-6 were used to detect differentially expressed miRNAs. Using miRNA microarray analysis and a computational approach, 17 cotton miRNAs belonging to eight families were identified. Although they are conserved, 12 of them showed a genotype-specific expression model in both the cultivars. Under salt stress treatment, miR156a/d/e, miR169, miR535a/b and miR827b were dramatically down-regulated in SN-011, while miR167a, miR397a/b and miR399a were up-regulated. Only miR159 was found to be down-regulated in LM-6 under salt stress. To gain insight into their functional significance, 26 target genes were predicted and their functional similarity was further analyzed. Quantitative real-time PCR showed that the expression of seven target genes showed a significant inverse correlation with corresponding miRNAs. These differentially expressed miRNAs can help in further study into the role of transcriptome homeostasis in the adaptation responses of cotton to salt.