tlr4

TLR4-IN-C34 is an inhibitor of TLR4, and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis

IAXO-102 is a TLR4 antagonist that negatively regulates TLR4 signaling by inhibiting MAPK and p65 NF-κB phosphorylation, as well as the expression of TLR4-dependent proinflammatory proteins. It also prevents the development of experimental abdominal aortic aneurysm.

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.

Rabeximod is a potent immunomodulator that reduces the severity of autoimmune diseases in rat models. Rabeximod inhibits arthritis in a time-dependent manner by stimulating TLR2 and TLR4 downstream to block the activation of inflammatory cells, most likely macrophages. Rabeximod effectively reduces brain antigen presentation in mice during anti-inflammatory therapy for traumatic brain injury.

Chloranil (tetrachloro-p-benzoquinone) triggers inflammation and neurological dysfunction through Toll-like receptor 4 signaling and can be used to model inflammation in mice.

Semapimod tetrahydrochloride (CPSI-2364 tetrahydrochloride) is a synthetic ornithine mitogen-activated protein kinase blocker and pro-inflammatory cytokine production inhibitor that interferes with macrophage and microglia function. Sematimod tetrahydrochloride inhibits TLR4 signaling, TNF-α, IL-1β, and IL-6, and is used in the study of Crohn's disease and other inflammatory conditions.

TLR4 inhibitor. Inhibits LPS-induced NF-κB activation in HEK293 cells (IC50 = 2.4 μg/mL). Also inhibits LPS-induced cytokine production and procoagulant effects in PBMCs and HUVECs. Prolongs survival in a mouse septic shock model.

Sparstolonin B, a selective TLR2 and TLR4 antagonist, is an isocoumarin compound isolated from the tubers of Sparganium stoloniferum and Scirpus yagara with anti-HIV, anticancer, antitumour and anti-inflammatory activities, inhibits selective Toll-like receptors, inhibits free fatty acids It inhibits selective Toll-like receptors, inhibits free fatty acid palmitate-induced chondrocyte inflammation and attenuates post-traumatic arthritis in obese mice, and inhibits lipopolysaccharide-induced inflammation in 3T3-L1 adipocytes, which can be used for validation and mammary carcinoma studies.

Kdo2-Lipid A ammonium (KLA) is a selective and potent TLR4 agonist, a lipopolysaccharide.Kdo2-Lipid A ammonium induces the release of TNF and PGE2.

1. Isofraxidin (Phytodolor) protects leukemia cells from radiation-induced apoptosis via ROS mitochondria pathway in a p53-independent manner. 2. Isofraxidin has a protective effect against LPS-induced ALI, and the protective effect of Isofraxidin seems to result from the inhibition of COX-2 protein expression in the lung, which regulates the production of PGE2. 3. Isofraxidin possesses significant analgesic and anti-inflammatory activities that may be mediated through the regulation of pro-inflammatory cytokines, TNF-α and the phosphorylation of p38 and ERK1 2.

Okanin shows significant activities on both linoleic acid peroxidation inhibition and DPPH radical scavenging effect.

TLR4 agonist. Promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. Acts as an adjuvant in vivo; enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.

RS09 2TFA (1449566-36-2 free base) is a TLR4 agonist. Promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. It acts as an adjuvant in vivo and enhances X-15 specific antibody serum concentrations.

TLR4-IN-1 (compound 3k) demonstrates potent inhibition of RAW264.7 cell viability with an IC 50 value of 1.02 μM. Additionally, it suppresses the release of cytokines TNF-α, IL-1β, and IL-6, and shows anti-inflammatory effectiveness in rat models of rheumatoid arthritis.

TLR4 NF-κB-IN-1 (Compound 7x) is an orally bioavailable inhibitor targeting the TLR4 NF-κB signaling pathway, with anti-inflammatory properties and the ability to cross the blood-brain barrier. It can alleviate LPS-induced acute neuroinflammation in mice and downregulate the protein expression of TLR4, P-NF-κB, and P-IκB-α.

TLR4-IN-C34-C2-COO is a linker compound incorporating the TLR4 inhibitor TLR4-IN-C34, effectively inhibiting TLR4 activity in enterocytes and macrophages, and mitigating systemic inflammation in murine models of endotoxemia and necrotizing enterocolitis.

TLR4 NF-κB MAPK-IN-1 is a novel antineuroinflammatory agent inhibiting the TLR4 NF-κB MAPK pathways.

TLR4-IN-C34-C2-amide-C6-OH, a chemical compound, functions as a linker incorporating the TLR4 inhibitor TLR4-IN-C34. This inhibitor targets TLR4 in enterocytes and macrophages, effectively reducing systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis [1].

Tri(TLR4-IN-C34-C2-amide-PEG1)-amide-C3-COOH is a chemical linker with the TLR4 inhibitor TLR4-IN-C34, which inhibits TLR4 in enterocytes and macrophages, reducing systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis [1].

Tri(TLR4-IN-C34-PEG2-amide-PEG1)-amide-C3-COOH is a chemical linker incorporating the TLR4 inhibitor (TLR4-IN-C34) that suppresses TLR4 activity in enterocytes and macrophages, consequently diminishing systemic inflammation observed in mouse models of endotoxemia and necrotizing enterocolitis [1].

Tri(TLR4-IN-C34-C2-amide-C3-amide-PEG1)-amide-C3-COOH, a chemical compound that serves as a linker incorporating TLR4 inhibitor TLR4-IN-C34, effectively inhibits TLR4 in both enterocytes and macrophages, significantly reducing systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis [1].

MD2-TLR4-IN-1 is a myeloid differentiation protein 2 toll-like receptor 4 (MD2-TLR4) complex inhibitor.

TLR4 agonist-1 (TEA, compound 17a) is a potent activator of Toll-like Receptor 4 (TLR4) and prompts the production of MIP-1β in RAW 264.7 and MM6 cells [1].

TLR4 agonist-1 (compound 17a) is a potent activator of Toll-like Receptor 4 (TLR4), stimulating MIP-1β production in RAW 264.7 and MM6 cells [1].