myd88

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.

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.

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.

ERK-MYD88 Interaction Inhibitor 1, an agent that disrupts the interaction between ERK and MYD88, has demonstrated the ability to trigger an HRI-mediated integrated stress response (ISR) that specifically promotes immunogenic cell apoptosis (apoptosis) in cancer cells. Additionally, in models using Lewis lung cancer mice, this compound has been shown to stimulate anti-tumor T cell responses, thereby exhibiting significant anti-tumor activity.

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.

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).

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.

Schaftoside (APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE) has antioxidant and anticancer activity.

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].

TJ-M2010-5 is a MyD88 inhibitor that binds to the TIR domain to interfere with its homodimerization and suppress MyD88 signaling. TJ-M2010-5 can be used in myocardial [ischemia reperfusion] injury studies.

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).

Pepinh-MYD, a MyD88 inhibitor, incorporates both a domain sequence from MyD88 TIR and a protein transduction sequence to facilitate cell membrane penetration. This compound disrupts MyD88-mediated TLR signaling pathways, effectively inhibiting associated immune responses. Its design is particularly useful for investigating MyD88's function in viral infections.

IRAK4-IN-10 (compound 75) is a potent IRAK4 inhibitor (IC50 = 1.5 nM) that can block the MyD88-dependent signaling pathway and has research potential in inflammatory diseases, autoimmune diseases, and cancer.

1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reduction of pro-inflammatory cytokines and LPS. 2. Atractylenolide-I significantly sensitizes the res

KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM for IRAK4 and 5 nM for Ikaros. It effectively induces apoptosis in MYD88 MT DLBCL and has demonstrated efficacy in inducing in vivo tumor regressions in a lymphoma model [1] [2] [3].

RDR 02308 is a TLR4-MyD88 binding inhibitor that inhibits full-length β-lactamase [1].

Artemisinin B is a drug which may improve spatial memory in dementia patients and alter the levels of inflammatory cytokines in the hippocampus and the cortex. Artemisinin B may inhibit neuroinflammation and exert neuroprotective effects on cognitive functions by modulating the TLR4-MyD88-NF-κB signaling pathway. Artemisinin B has shown potential in the treatment of neuroinflammatory diseases.

TSI-13-57 is a MyD88 inhibitor.

D-Mannuronic Acid is a blocker of the TLR2 and TLR4 downstream signaling pathway. D-Mannuronic Acid effectively inhibits mRNA expression of MyD88 and p65, major subunit of nuclear factor-kappaB.

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

IRAK4-IN-6 is a selective and orally efficacious inhibitor of IRAK4, demonstrating an IC50 value of 4 nM. This compound specifically targets MyD88 L265P mutant diffuse large B-cell lymphoma [1].

ST 2825 is a specific MyD88 dimerization inhibitor that blocks IL-1β-mediated activation of NF-κB transcriptional activity.

IRAK4-IN-14 is a selective, potent, orally active IRAK4 inhibitor (IC50: 0.003 μM) with favorable PK parameters in rats and mice. effect.