tlr4

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

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) serves as a potent activator of Toll-like Receptor 4 (TLR4) and stimulates the production of MIP-1β in RAW 264.7 and MM6 cells [1].

Tri(TLR4-IN-C34-C2-amide-PEG1)-amide-C3-COOH is a chemical linker featuring the TLR4 inhibitor TLR4-IN-C34, known for inhibition of TLR4 in enterocytes and macrophages, thereby diminishing systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis [1].

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

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

TLR4-IN-C34-C2-amide-C6-OH, a chemical compound, serves as a linker encompassing the TLR4 inhibitor TLR4-IN-C34. This inhibitor is known to target TLR4 in enterocytes and macrophages, effectively 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-IN-C34-C2-COO is a linker compound that incorporates TLR4 inhibitor TLR4-IN-C34. It effectively inhibits TLR4 activity in enterocytes and macrophages. Moreover, it demonstrates a notable ability to mitigate systemic inflammation in murine models of endotoxemia and necrotizing enterocolitis.

RV01 is a novel quinoline-substituted analogue of resveratrol that inhibits DNA damage, reduces ethanol-induced acetaldehyde dehydrogenase (ALDH2) mRNA expression, and has hydroxyl radical scavenging activity. rV01 reduces iNOS expression and has anti-neuroinflammatory effects. rV01 reduces tumor necrosis factor-a (TNF-a) and interleukin-6 (IL-6) mRNA levels and secretion. RV01 reduced tumor necrosis factor-a (TNF-a) and interleukin-6 (IL-6) mRNA levels and secretion, inhibited lps-induced ROS production and nicotinamide adenine dinucleotide phosphate (NADPH) oxidase activation, decreased toll-like receptor 4 (TLR4) protein expression, and inhibited lps-induced activation of mitogen-activated protein kinase (MAPK) and nuclear transcription factor-кB (NF-кB) signaling pathways.

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.

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.

4-methoxylonchocarpin was isolated from the roots of Abrus precatorius as a potent anti-inflammatory compound. 4-methoxylonchocarpin inhibited NF-κB-activated TNF expression by inhibiting the binding of LPS to TLR4 in macrophages and suppressed TNBS-induced colitis in mice.

ABR-238901 is an oral, active S100A8/A9 blocker that inhibits the interaction of S100A8/A9 with its receptors RAGE(receptor for advanced glycation end products) and TLR4 (toll-like receptor 4). ABR-238901 has potential as a compound for the treatment of myocardial infarction (MI).

Enpatoran is an inhibitor of TLR7(IC50 = 11.1 nM) and TLR8(IC50 = 24.1 nM). Enpatoran was found to be inactive against TLR3, TLR4, and TLR9 in vitro and in vivo.

Inflachromene (ICM) is an inhibitor of HMGB1 and HMGB expression with anti-inflammatory activity.Inflachromene reduces seizure severity in a mouse model of epilepsy by inhibiting HMGB1 translocation, inhibits endothelial proliferation through the HMGB1/2-regulated TLR4-NF-κB pathway, and inhibits autophagy by regulating Beclin 1 activity. Inflachromene can be used to study epilepsy.

Polygalasaponin F has anti-neuroinflammatory activity, can inhibit the release of inflammatory cytokines TNF-α and NO induced by lipopolysaccharides (LPS) and reduce the expression of inducible nitric oxide synthases. Polygalasaponin F can significantly i

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

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

Resatorvid (TAK-242) is a selective inhibitor of Toll-like receptor 4 (TLR4). Resatorvid binds directly to Cys747 and prevents TLR4 from binding to TIRAP, thereby blocking downstream signaling. Resatorvid has antitumor activity, anti-inflammatory activity, and neuroprotective effects.

RS 09 TFA, a TLR4 agonist, promotes NF-κB nuclear translocation and induces the secretion of inflammatory cytokines in RAW264.7 macrophages in vitro. Additionally, as an adjuvant in vivo, RS 09 TFA enhances serum concentrations of X-15 specific antibodies when co-administered with X-15-KLH in mice.

PSMα3 TFA is a peptide utilized in directing dendritic cells (DCs) towards a tolerogenic state, pivotal for DC vaccination approaches. It intrudes and recalibrates human monocyte-derived DCs, disrupting maturation triggered by TLR2 or TLR4, suppressing both pro-inflammatory and anti-inflammatory cytokine secretion, and diminishing antigen assimilation. Notably, PSMα3 TFA constitutes a significant toxin secreted by highly virulent methicillin-resistant Staphylococcus aureus (MRSA) strains [1] [2].

IAXO-101 interferes with TLR4/CD14 signals in humans, rats, and mice.

Chitohexaose hexahydrochloride is a chitosan oligosaccharide compound that possesses anti-inflammatory properties. It exerts its anti-inflammatory effect by binding to the active sites of TLR4, thereby inhibiting inflammation induced by LPS. This compound has been supported by references [1] and [2].

GSK1795091 (CRX-601) is a synthetic TLR4 agonist and immunologic stimulator with demonstrated antitumor activity. It serves as a vaccine adjuvant, enhancing both mucosal and systemic immunity to influenza virus vaccines.

PSMα3 is a peptide compound that can be utilized to induce tolerance in dendritic cells (DCs) for DC vaccination strategies. It effectively penetrates and modulates human monocyte-derived DCs by modifying the maturation process induced by TLR2 or TLR4. Additionally, PSMα3 inhibits the production of both pro- and anti-inflammatory cytokines and decreases antigen uptake. Notably, PSMα3 is a significant virulence factor released by the most pathogenic strains of methicillin-resistant Staphylococcus aureus (MRSA).

Capillarisin is a novel blocker of STAT3 activation and thus may have a potential in negative regulation of growth, metastasis, and chemoresistance of tumor cells, it inhibits cancer cell growth of osteosarcoma cells by inducing apoptosis accompanied with

Eritoran, a Toll-like receptor 4 (TLR4) antagonist, effectively protects mice from lethal infections caused by viruses such as the Ebola virus (EBOV) and Marburg virus (MARV). By decreasing granulocytosis levels, Eritoran may reduce the severity of cytokine storms, thereby inhibiting the pathogenesis of filovirus infections [1].

CAY10614 is a TLR4 antagonist. CAY10614 inhibits lipid A-induced activation of TLR4 (IC50=1.675 μM). CAY10614 also improves survival in LPS-induced shock model mice.

AZ617 is a potent agonist of TLR4.

CRX-526, a TLR4 antagonist, protects against advanced diabetic nephropathy.

L-asarinin ((-)-Episesamin) reduces peripheral blood concentration of IL-12 and inhibits the expression of CXCR3 and TLR4, which means Asarinin may have a role on the TLR4 pathway and produce prolongation of allograft heart survival.

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.

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.

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

1. Schisandrol B (Besigomsin) may exert neuroprotective effects by attenuating the microglia-mediated neuroinflammatory response via inhibiting the TLR4-mediated NF-κB and MAPKs signaling pathways. 2. Schisandrol B has anti-inflammatory property, potentially result from the inhibition of COX-2, iNOS, IL-6, TNF-α and NO through the down-regulation of RIP2 and NF-κB activation. 3. Schisandrol B induces marked protective effects against hepatic and renal injury induced by CCl(4) exposure through differential regulation of the MAPK signal transduction pathway. 4. Schisandrol B significantly inhibits cell proliferation in a dose-dependent manner, due to cell cycle arrest in the G1 phase with the downregulation of cyclin D1 expression and Retinoblastoma (RB) phosphorylation.

Simufilam dihydrochloride (PTI-125 dihydrochloride) is a low toxicity, orally active filamin A (FLNA) activator, which can be used for the research of Alzheimer's disease. Simufilam dihydrochloride preferentially binds altered FLNA and restores its native conformation, restoring receptor and synaptic activities and reducing its α7nAChR/TLR4 associations and downstream pathologies.

L6H21 is an inhibitor of the interaction and signaling transduction of LPS-TLR4/MD-2 (myeloid differentiation 2).

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.

Simufilam (PTI-125) (hydrochloride) is an orally active filamin A (FLNA) activator with low toxicity that can be used in the Alzheimer's disease research. Simufilam (hydrochloride) preferentially binds to altered FLNA and restores its native conformation, restores receptor and synaptic activities, and reduces its a7nAChR/TLR4 associations and downstream pathologies [1].

IAXO-102 is a TLR4 antagonist that negatively regulates TLR4 signaling. It inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein. IAXO-102 also prevents experimental abdominal aortic aneurysm development.

Semapimod is an inhibitor of proinflammatory cytokine production, capable of suppressing TNF-α, IL-1β, and IL-6. It hinders TLR4 signaling with an IC50 of approximately 0.3 μM, impedes p38 MAPK, and reduces nitric oxide production in macrophages. This compound shows promise for treating various inflammatory and autoimmune disorders [1] [2] [3].

NCI 126224, a toll-like receptor 4 (TLR4) antagonist, demonstrates selective inhibition of nitric oxide (NO) production in RAW 264.7 macrophages, triggered by the TLR4 agonist LPS (IC50 = 0.31 µM), as opposed to minimal effects on NO production induced by agonists for TLR7/8 (R-848), TLR1/2 (Pam3CSK4), and TLR3 (poly(I:C)). Nevertheless, it also effectively inhibits NO production initiated by the TLR2/6 agonist FSL-1 at an IC50 of 0.6 µM in the same cell line. Moreover, NCI 126224 suppresses LPS-induced NF-κB activity in BV-2 microglial cells and reduces LPS-triggered increases in IL-1β and TNF-α levels in RAW 264.7 macrophages with IC50 values of 5.92, 0.42, and 1.54 µM, respectively.

Eritoran Tetrasodium, a TLR4 receptor antagonist, is used potentially for the treatment of type 2 diabetes.

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.

Antimicrobial Agent-5 is a potent antimicrobial agent that exhibits exceptional cell selectivity against both Gram-negative and Gram-positive bacteria. It inhibits the interaction between LPS (lipopolysaccharide) and the CD14/TLR4 (Toll-like receptor 4) receptor, demonstrating anti-inflammatory activity in combating LPS-induced inflammation.

Protosappanin A (PTA) has anti-oxidative/nitrative activities on brain immune and neuroinflammation through regulation of CD14/TLR4-dependent IKK/IκB/NF-κB inflammation signal pathway; it exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia. Protosappanin A induces immunosuppression of rats heart transplantation targeting T cells in grafts via NF-kappaB pathway. Protosappanin A and protosappanin B have antimicrobial activity, they show both alone activities and resistance reversal effects of amikacin and gentamicin against MRSA. Protosappanin A shows strong effect against HIV-1 IN with an IC50 value of 12.6 uM.

IRAK4-IN-7 (CA-4948) is a selective and potent IRAK4 kinase inhibitor with in vivo activity in a TLR4-induced cytokine release model.

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