STING-IN-4 (Compound 1) 是一种STING抑制剂，抑制 STING 的表达，从而降低 STING 和核因子-κB (NF-κB) 信号通路的激活。STING-IN-4 具有抗炎活性，可用于脓毒症的研究。
| 生物活性 | STING-IN-4 (Compound 1) is aSTINGinhibitor that inhibitsSTINGexpression and hence reducing activation ofSTINGand nuclear factor-κB (NF-κB) signaling. STING-IN-4 shows anti-inflammatory activity and can be used for the research of sepsis[1]. |
| IC50& Target | |
体外研究
(In Vitro) | STING-IN-4 (Compound 1) (20 μM; 26 h) 抑制 LPS 诱导 RAW264.7 细胞产生 NO[1]。
STING-IN-4 (2.5-10 μM; 26 h) 显著抑制 RAW264.7 细胞中 iNOS 的表达[1]。
STING-IN-4 (5 and 50 μM; 12 h) 在 49、52 和 55 ℃时显著降低 STING 的降解，并可能与 STING 相互作用并增强 STING 的热稳定性[1]。
STING-IN-4 (2.5-10 μM; 8 h) 抑制 LPS 诱导的 STING/IRF3/NF-κB 的激活[1]。
Western Blot Analysis[1] | Cell Line: | RAW264.7 cells | | Concentration: | 2.5, 5 and 10 μM | | Incubation Time: | Pre-treated for 2 h followed LPS treatment for 6 h or 24 h | | Result: | Inhibited the expression of iNOS (24 h). Blocked LPS-induced phosphorylation of TBK1, IRF3, p65, and IκB-α (6 h). |
|
体内研究
(In Vivo) | STING-IN-4 (Compound 1) (1-9 mg/kg; i.p.; daily for 3 days) 保护 LPS 诱导的小鼠肝损伤，抑制脓毒症小鼠肝脏 STING/IRF3/NF-κB 激活[1]。
| Animal Model: | BALB/c mice, LPS-induced acute liver injury model[1] | | Dosage: | 1, 3 and 9 mg/kg | | Administration: | Intraperitoneal injection, daily for 3 days | | Result: | Significantly reduced the hemorrhage severity. Decreased the levels of alanine transaminase (ALT), aspartate aminotransferase (AST), and alkaline phosphatase (ALP) induced by LPS. Significantly reduced the levels of TNF-α, IL-6, and IFN-β compared with mice treated only with LPS. Markedly reduced the levels of STING, p-TBK, p-IRF3, p-p65, and p-IκB-α. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
