TH1020 is a potent, selective antagonist of TLR5/flagellin protein-protein interaction with IC50 of 0.85 uM.
TH1020 exhibits nearly negligible inhibition of TLR2, TLT4, TLR7 and TLR8 at 0.78 uM, and weak inhibition of TLR3.
TH1020 represses the expression of downstream TNF-α signaling pathways mediated by the TLR5/flagellin complex formation.
TH1020 almost completely abolishes the TLR5-mediated TNF-α secretion at 0.37 uM in primary human peripheral blood mononuclear cells (PBMCs).
