LB244 is an irreversible STING antagonist.[1] It binds to STING in a cell-free assay and inhibits STING activation induced by the STING agonist diABZI in cells (EC50 = 0.8 nM). LB244 (1 µM) inhibits diABZI-induced STING oligomerization and phosphorylation of IFN regulatory factor 3 (IRF3) and TANK-binding kinase 1 (TBK1) in primary mouse bone marrow-derived macrophages (BMDMs). In vivo, LB244 (5 mg/kg, i.p.) reduces diABZI-induced increases in serum IL-6 and IFN-β levels in mice.
References:
[1].Barasa, L., Chaudhuri, S., Zhou, J.Y., et al.Development of LB244, an irreversible STING antagonistJ. Am. Chem. Soc.145(37)20273-20288(2023).