STING-IN-5 is a potent STING inhibitor, inhibiting LPS-induced NO synthesis in macrophages with an IC50 value of 1.15 μM. STING-IN-5 inhibits the inflammatory response. STING-IN-5 can be used to research anti-inflammatory diseases and sepsis.
STING-IN-5 (compound 30) (40 μM; 24 h) exhibits less effect on RAW264.7 cell viability[1].
STING-IN-5 (2.5 and 5 μM; 2 h) inhibits NO production in LPS-stimulated RAW264.7 with inhibition rate of 69.28 ± 2.36 and 78.66 ± 2.73 at 2.5 and 5 μM, respectively, and exhibits IC50 of 1.15 ± 0.15 μM[1].
STING-IN-5 (0.5-2 μM; 2 h) suppresses STING, as well as TBK1/IRF3/NF-κB activation[1].
STING-IN-5 (1.25-5 mg/kg; i.g.; once daily; for 3 days) have an obvious protective effect on acute liver injury in septic mice[1].
Pharmacokinetic Parameters of STING-IN-5 in male Sprague-Dawley rats[1].
| Tmax (h) | Cmax (ng/mL) | AUC0-t (ng/mL·h) | AUC0-∞ (ng/mL·h) | T1/2 (h) | MRT0-t (h) | MRT0-∞ (h) |
| 1 | 66.52 | 81.08 | 135.7 | 1.11 | 0.99 | 2.02 |
References:
[1]. Long J, et al. Discovery of fusidic acid derivatives as novel STING inhibitors for treatment of sepsis. Eur J Med Chem. 2022 Dec 15;244:114814.