TLR2

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.

A natural, noncaloric sweetener with a potency 300 times more than that of regular sucrose. Exhibits transepithelial p-aminohippurate transport via organic anion transport system interference.

Valsartan (CGP 48933) is a tetrazole derivative and angiotensin II type 1 receptor blocker that is used to treat hypertension.

CU-T12-9 is a potent TLR1/2 agonist(EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay). It acts by activating the NFkB pathway, upregulating proinflammatory cytokines, and enhancing TLR1 and TLR2 dimerization.CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.

MMG-11 inhibits both TLR2/1 and TLR2/6 signaling (IC50s: 1.7 μM for Pam3CSK4-induced hTLR2/1 and 5.7 μM for Pam2CSK4-induced hTLR2/6 responses). MMG-11 is an effective and selective human TLR2 antagonist with low cytotoxicity.

C29 is a novel inhibitor of TLR2/1 and TLR2/6 signaling induced by synthetic and bacterial TLR2 agonists in human HEK-TLR2 and THP-1 cells, but only TLR2/1 signaling in murine macrophages.

Corilagin has anti-inflammatory activity. Corilagin has a significant antitumour potential and lower toxicity in normal cells in vitro.Corilagin can enhance the cytotoxicity of both cisplatin and doxorubicin on the Hep3B hepatoma cells.Corilagin has antiviral activity, reduces the cytotoxicity induced by EV71 or CA16 on Vero cells with and IC50 value of 5.6 and 32.33 μg/mL, respectively. Corilagin shows the potential to protect against HSV-1-induced encephalitis, and the beneficial effects may be mediated by inhibiting TLR2 signaling pathways.Corilagin has antifibrotics property and is potentiated in treating idiopathic pulmonary fibrosis(IPF), attenuates bleomycin-induced epithelial injury and fibrosis via inactivation of oxidative stress, proinflammatory cytokine release and NF-κB and TGF-β1 signaling. Solvent:Pyridine, Methanol, Ethanol, etc.

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.

Tomaralimab (OPN-305) is a humanized IgG4 monoclonal antibody targeting TLR2, used to study myelodysplastic syndromes (MDS).

Pam2CSK4 TFA (PUL-042 TFA) is a potent dual agonist of TLR2 and TLR6, a peptide that mimics bacterial lipoproteins.Pam2CSK4 TFA promotes platelet aggregation, and can be used to study the effects of lipoproteins on the periodontium.

CU-CPT22 is the first probe for the complex between toll-like receptors TLR1 and TLR2. CU-CPT22 binds at the interface of TLR1 and TLR2 (IC50 = 0.58 μM). It competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 (Ki: 0.41 μM).

GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor that inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells[1]. It blocks the synergy between NOD2 and TLR2 without affecting NOD1, TNFR1, and TLR2-mediated responses. At 5 μM, GSK717 inhibits the release of IL-8, IL-6, TNFα, and IL-1β in primary human monocytes stimulated with MDP[1]. [1]. Rickard DJ, et al. Identification of benzimidazole diamides as selective inhibitors of the nucleotide-binding oligomerization domain 2 (NOD2) signaling pathway. PLoS One. 2013;8(8):e69619. Published 2013 Aug 1.

Pam3CSK4 TFA (Pam3Cys-Ser-(Lys)4 TFA) is a Toll-like receptor 1/2 agonist with EC50 of 0.47 ng/mL for human TLR1/2.

P53/TLR2 modulator-1 (Compound Z9) is an agent that targets both the P53 pathway and TLR2, exhibiting radioprotective properties. It mitigates apoptosis by inhibiting radiation-induced expression of P53 and Bax. Concurrently, it enhances the TLR2 pathway by upregulating downstream proteins MyD88 and P65, which promotes secretion of cytokines like IL-6, providing radioprotective effects. P53/TLR2 modulator-1 shows significant radioprotective activity in AHH-1 and HUVECs cells, enhances survival rates in C57BL/6J mice exposed to lethal radiation doses, and alleviates radiation-induced damage to their hematopoietic system, intestinal villi, and spleen. It is applicable for research on radiation-related diseases.

TLR2antagonist-1 is a selective antagonist of Toll-like receptor 2 (TLR2). It effectively inhibits excessive activation of TLR2, with an IC50 value of 11.41 μM, and reduces the production of inflammatory factors. TLR2antagonist-1 exhibits metabolic stability, with a half-life (T1/2) of 16.67 minutes in mouse liver microsomes. This compound is useful for research in inflammation, immunology, and neurological disorders.

TLR2/9 antagonist 1 (Compound 24) is a reversible covalent antagonist of TLR2, with an IC₅₀ of 0.5 μM for TLR2/TLR6 and 0.6 μM for TLR2/TLR1, as well as TLR9, with an IC₅₀ of 0.32 μM. This compound does not significantly affect other TLR subtypes and is utilized for studying central nervous system diseases and malignancies caused by inflammation.

The TLR2Pig Pre-designed siRNA Set A comprises three pairs of siRNAs designed to target different regions of the TLR2(Pig) gene. It also includes a negative control, a FAM-labeled negative control, and a positive control.

TLR2 Agonist1 (Compound R-7d) serves as an activator for human toll-like receptor 2 (TLR 2) with an EC50 of 116 pM. It enhances the activation of the NF-κB promoter via the TLR2/TLR1 heterodimer.

Creatine ethyl ester (CEE) is a readily available form of creatine commonly used in supplements. It can upregulate TLRs (TLR2, 3, 4, and TLR7) over a short period.

LPS-PG is a lipopolysaccharide from Porphyromonas gingivalis (P. gingivalis). It functions as a crucial virulence factor in the pathogenesis of periodontal disease by activating immune cells through Toll-like receptor 2 (TLR2), rather than the Escherichia coli (E. coli) receptor, Toll-like receptor 4 (TLR4). A lipoprotein from LPS-PG has been identified as the primary component responsible for TLR2-mediated cell activation.

a15:0-i15:0 PE is a dia-cyl phosphatidylethanolamine with two branched chains. It functions as an atypical TLR2-TLR1 heterodimer agonist and is immunogenic. This compound activates T cell and dendritic cell (DC) signaling, exhibiting anti-inflammatory properties. Additionally, a15:0-i15:0 PE induces the production of TNFα and IL-6. It is a major component of the A. muciniphila lipid membrane, constituting approximately 50%.

ETI60 is an orally active selective TLR inhibitor that targets the nucleoside-binding sites I of TLR7 (IC50 = 0.68 μM) and TLR9 (IC50 = 0.12 μM) without affecting surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4, and TLR5). It demonstrates nanomolar activity in cell-based, biophysical, and in vivo assays, effectively inhibiting endosomal TLR-mediated pro-inflammatory signaling. ETI60 modulates the expression of genes related to inflammation and significantly improves symptoms in mouse models of psoriasis and systemic lupus erythematosus (SLE). ETI60 is applicable in studies related to autoimmune and inflammatory diseases.

ETI41 is an orally active selective TLR inhibitor that targets the nucleoside-binding site I of TLR7 (IC50= 0.63 μM) and TLR9 (IC50= 0.16 μM), without affecting surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4, and TLR5). It demonstrates nanomolar activity in cell-based, biophysical, and in vivo studies, effectively inhibiting endosomal TLR-mediated pro-inflammatory signaling. ETI41 suppresses the expression of inflammation-related genes and significantly improves symptoms in mouse models of psoriasis and systemic lupus erythematosus (SLE). ETI41 is applicable in research related to autoimmune and inflammatory diseases.

Ganglioside GT1b bovine trisodium is a trisialoganglioside that binds to botulinum toxin type A (BTxA), BTxA heavy chain, and tetanus toxin with IC50 values of 11, 0.74, and 7.2 μM, respectively. It acts as a TLR2 agonist in spinal cord microglia, leading to microglial activation, increased expression of pro-inflammatory factors, and heightened pain sensitivity. Additionally, Ganglioside GT1b bovine trisodium reduces the production of IL-6, IL-10, IgG, IgM, and IgA in human peripheral blood mononuclear cells (PBMC). In neuronal cell models, it elevates extracellular glutamate levels. Ganglioside GT1b bovine trisodium is used in the research of immune and neurological disorders.