htlr2/6

CU-T12-9 is a potent TLR1 2 agonist(EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay). It acts by activating the NFkB pathway, upregulating proinflammatory cytokines, and enhancing TLR1 and TLR2 dimerization.CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1 2 heterodimer, not TLR2 6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.

C29 is a novel inhibitor of TLR2 1 and TLR2 6 signaling induced by synthetic and bacterial TLR2 agonists in human HEK-TLR2 and THP-1 cells, but only TLR2 1 signaling in murine macrophages.

MMG-11 inhibits both TLR2 1 and TLR2 6 signaling (IC50s: 1.7 μM for Pam3CSK4-induced hTLR2 1 and 5.7 μM for Pam2CSK4-induced hTLR2 6 responses). MMG-11 is an effective and selective human TLR2 antagonist with low cytotoxicity.

MMG-11 quarterhydrate is a potent and selective antagonist of human TLR2, inhibiting both TLR2 1 and TLR2 6 signaling with low cytotoxicity. The IC50 values for Pam3CSK4-induced hTLR2 1 and Pam2CSK4-induced hTLR2 6 responses are 1.7 μM and 5.7 μM, respectively [1].