C-178,STING 的共价抑制剂,与 Cys91 有效结合并选择性地抑制小鼠中不同的激活剂引起的 STING 反应。C-178 选择性地降低 STING- 而非 RIG-I- 或 TBK1- 介导的 IFN-β 报告基因活性。C-178 阻断棕榈酰化 (PMA) 诱导的 STING 类聚;抑制 CMA 诱导的 TBK1 (STING 下游蛋白激酶) 磷酸化。
Cas No. | 329198-87-0 |
别名 | N-(二苯并[B,D]呋喃-3-基)-5-硝基呋喃-2-甲酰胺 |
Canonical SMILES | O=C(C1=CC=C([N+]([O-])=O)O1)NC2=CC=C3C(OC4=CC=CC=C34)=C2 |
分子式 | C17H10N2O5 |
分子量 | 322.27 |
溶解度 | DMSO: 41.67 mg/mL (129.30 mM) |
储存条件 | Store at -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 | C-178, a covalent inhibitor of STING, binds to Cys91, potently and selectively suppresses the STING responses elicited by distinct bona fide activators in mouse but not human. C-178 significantly reduces STING-, but not RIG-I- or TBK1-, mediated IFN-β reporter activity. C-178 blocks palmitoylation (PMA)-induced clustering of STING; inhibits the CMA-induced phosphorylation of TBK1 (downstream protein kinase of STING)[1]. [1]. Haag SM, et al. Targeting STING with covalent small-molecule inhibitors. Nature. 2018 Jul;559(7713):269-273. |