myd 88

Resatorvid (TAK-242), a selective Toll-like receptor 4 (TLR4) inhibitor, binds directly to Cys747 to prevent TLR4-TIRAP interaction, thereby blocking downstream signaling. Resatorvid exhibits antitumor, anti-inflammatory, and neuroprotective activities.

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.

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

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].

D228, a natural product from Chimonanthus salicifolius, is an orally available anti-inflammatory agent with favorable inhibitory activity on B and T lymphocytes, down-regulation of MyD88 TRAF6 p38 and up-regulation of IL-10 to reduce inflammation, and can be used for the treatment of inflammatory bowel disease (IBD).

MyD88-IN-2 (compound A5S) is a MyD88 inhibitor with a Kd value of 15 μM. It demonstrates protective effects in mouse models of acute lung injury induced by LPS and sepsis.

Pepinh-MYD TFA is a MyD88 inhibitor that features domain sequences from MyD88TIR and a protein transduction sequence, allowing it to penetrate cell membranes. By disrupting MyD88-mediated TLR pathway signaling, it inhibits related immune responses. Pepinh-MYD TFA shows potential for investigating MyD88's role in viral infections.

CL075 (3M002) is a selective TLR8 agonist with immunomodulatory activity, triggering the MyD88-dependent signaling pathway and activating NF-κB and IRF7 to elicit the production of inflammatory cytokines and type I interferon (IFN).

CA-4948 (Emavusertib) is a potent IRAK4 FLT3 inhibtor. CA-4948 with anti-tumor activity.

JH-X-119-01 is a highly potent and selective covalent inhibitor of IRAK-1 (Interleukin-1 Receptor-Associated Kinase 1).