STING-IN-4

STING-IN-4 (Compound 1) is a STING inhibitor that inhibits STING expression and hence reducing activation of STING and nuclear factor-κB (NF-κB) signaling. STING-IN-4 shows anti-inflammatory activity and can be used for the research of sepsis[1].

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Immunology/Inflammation >> STING

STING[1]

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 °C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).

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.

[1]. Yu T, et al. Design and synthesis of hederagenin derivatives modulating STING/NF-κB signaling for the relief of acute liver injury in septic mice. Eur J Med Chem. 2023 Jan 5;245(Pt 1):114911.