TLR1 is a cell-penetrating Toll/IL-1 receptor/resistance (TIR) domain/BB-Loop mimic and inhibits IL-1 receptor-mediated responses.

MyD88-IN-1 is a potent MyD88 inhibitor with anti-inflammatory activity, inhibiting downstream pathways such as the NF-κB pathway of the Toll-like receptor (TLR) and interleukin-1 (IL-1) receptor family. MyD88-IN-1 may be used in the study of cancer and inflammation treatment.

EM 163 is a TIR-TIR interaction inhibitor, which is a TIR (Toll/interleukin-1 receptor) structural domain mimic of the MyD88 protein. EM 163 targets the TIR structural domain in the IL-1 receptor and blocks the interaction with MyD88. EM 163 inhibits the production of inflammatory cytokines in vivo caused by staphylococcal enterotoxin B (SEB). EM 163 protects mice from SEB shock-induced death. In rat hippocampal neurons in vitro, EM 163 blocked the activation of p38 and the inhibitory effect of IL-1β on chemically induced long-term potentiation (LTP)-triggered protein synthesis.

T6167923 is a potent, selective inhibitor of MyD88-dependent signaling pathways. It achieves this by directly binding to the Toll/IL1 receptor (TIR) domain of MyD88, preventing MyD88 homodimer formation. Subsequently, T6167923 impedes NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity and boasts improved anti-inflammatory effects, with IC50s values of 2.7 μM for IFN-γ, 2.9 μM for IL-1β, and 2.66 μM each for IL-6 and TNF-α, demonstrating its efficacy across multiple inflammatory mediators [1].