E6446 is a novel orally available small molecule inhibitor of TLR7 and TLR9 with IC50 of 1.78 uM and 0.01 uM, respectively.
E6446 shows weak activity against TLR4 (IC50=10.58 uM).
E6446 potently inhibits IL-6 production induced by CpG2216 and suppresses both IL-6 and α-interferon production induced by CpG oligo.
E6446 prevents DNA-TLR9 interaction in vitro and modulates signaling in vivo.
