SN-011 是一种有效的选择性小鼠和人类 STING 抑制剂,对 STING 信号传导的 IC50 为 76 nM。
Cas No. | 2249435-90-1 |
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 | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | SN-011 is a stimulator of interferon genes (STING) antagonist.1It binds to the STING cyclic dinucleotide binding site (Kd= 4.03 nM) and inhibits 2’3’-cGAMP-inducedIfnbexpression 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 reducesIfnbmRNA levels in theTrex1-/-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) |