2. Signaling Pathways
  3. Immunology/Inflammation
  4. Toll-like Receptor (TLR)

Toll-like Receptor (TLR)

Toll-like Receptor (TLR)

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Toll-like receptors (TLRs) are a class of proteins that play a key role in the innate immune system. They are single, membrane-spanning, non-catalytic receptors usually expressed in sentinel cells such as macrophages and dendritic cells, that recognize structurally conserved molecules derived from microbes. Once these microbes have breached physical barriers such as the skin or intestinal tract mucosa, they are recognized by TLRs, which activate immune cell responses. The TLRs include TLR1, TLR2, TLR3, TLR4, TLR5, TLR6, TLR7, TLR8, TLR9, TLR10, TLR11, TLR12, and TLR13. Toll-Like Receptors (TLRs) play a critical role in the early innate immune response to invading pathogens by sensing microorganism and are involved in sensing endogenous danger signals. TLRs are evolutionarily conserved receptors are homologues of the Drosophila Toll protein, discovered to be important for defense against microbial infection. TLRs recognize highly conserved structural motifs known as pathogen-associated microbial patterns (PAMPs), which are exclusively expressed by microbial pathogens.

Toll-like Receptor (TLR) Isoform Specific Products:

Toll-like Receptor (TLR) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-D1056H
    Lipopolysaccharides, from S. marcescens
    		Activator
    Lipopolysaccharides, from S. marcescens (Serratia marcescens) are lipopolysaccharide endotoxins and TLR-4 activators derived from Serratia marcescens, classified as S-type LPS, which can activate pathogen-associated molecular patterns (PAMP) of the immune system and induce cellular secretion of migrasomes. Lipopolysaccharides, from S. marcescens exhibit a typical three-part structure: O-antigen (O-antigen), core oligosaccharide (core oligosaccharide), and lipid A (Lipid A). Lipopolysaccharides, from S. marcescens induce NF-κB activation in mouse cells via Toll-like receptor (TLR4)/MD-2. The lipopolysaccharides of S. marcescens can induce apoptosis in host immune cells, thereby suppressing the host's innate immunity.
    It is recommended to prepare a stock solution of ≥2 mg/mL and ensure that it is fully mixed and dissolved. Due to the adsorption characteristics of LPS, low adsorption centrifuge tubes should be used for aliquoting and storage.
    Lipopolysaccharides, from S. marcescens
  • HY-P10586A
    Macrophage-activating lipopeptide 2 TFA
    		Activator 98.60%
    Macrophage-activating lipopeptide 2 TFA is an agonist of Toll like receptors TLR-2/TLR-6. Macrophage-activating lipopeptide-2 enhances endothelial nitric oxide synthase (eNOS) phosphorylation and endothelial cell release of NO, thereby improving vasodilation. Macrophage-activating lipopeptide-2 enhances endothelial adhesion of white blood cells and improve perfusion recovery and collateral growth in the hind limbs of hypercholesterolemic Apoe deficient mice undergoing experimental femoral artery ligation (FAL).
    Macrophage-activating lipopeptide 2 TFA
  • HY-150745A
    ODN 24987 sodium
    ODN 24987 sodium is a Guanine-modified inhibitory oligonucleotides (ODN), targeting TLR9. ODN 24987 can inhibit IL-6 and IFN-α release. ODN 24987 sodium can be used for research immune disorders. ODN 24987 sequence: 5’-C-C-T-G-G-C-c7G-G-G-G-3’.
    ODN 24987 sodium
  • HY-125390
    SM-360320
    		Agonist 99.41%
    SM-360320 (CL-087) is a potent, orally active TLR7 agonist. SM-360320 is a immuno-modulator and exerts an antitumor effect. SM-360320 can act in synergy with DNA vaccines leading to an enhanced Th1 antibody response. SM-360320 can inhibit HCV replication in hepatocytes via a type I IFN-independent mechanism in addition to its IFN-mediated activity.
    SM-360320
  • HY-B0380A
    Trimebutine maleate
    		Inhibitor 99.91%
    Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
    Trimebutine maleate
  • HY-N0392
    Polygalasaponin F
    		Inhibitor 99.85%
    Polygalasaponin F, an oleanane-type triterpenoid saponin extracted from Polygala japonica, decreases the release of the inflammatory cytokine tumor necrosis factor a (TNFa). Polygalasaponin F reduces neuroinflammatory cytokine secretion through the regulation of the TLR4-PI3K/AKT-NF-kB signaling pathway .
    Polygalasaponin F
  • HY-D1056E
    Lipopolysaccharides, from P. aeruginosa 10
    		Activator
    Lipopolysaccharides from P. aeruginosa (Pseudomonas aeruginosa) 10 are lipopolysaccharide endotoxins and TLR4 activators derived from Pseudomonas aeruginosa 10, and are classified as S-type LPS. Lipopolysaccharides from P. aeruginosa 10 exhibit a typical three-part structure: O-antigen, core oligosaccharide, and lipid A. The lipopolysaccharides of P. aeruginosa 10 have a fatty acid composition distinct from common enterobacteria, an exceptionally high degree of phosphorylation (triphosphate residues have been detected), and a unique outer region of the core oligosaccharide. Additionally, their O-specific side chains are typically rich in novel aminosugars. Lipopolysaccharides from P. aeruginosa 10 demonstrate susceptibility to viruses, with the level of susceptibility determined by the content of high molecular weight polysaccharides in their composition. The absence of high molecular weight polysaccharides increases their sensitivity to bacteriophages.
    It is recommended to prepare a stock solution of ≥2 mg/mL and ensure that it is fully mixed and dissolved. Due to the adsorption characteristics of LPS, low adsorption centrifuge tubes should be used for aliquoting and storage.
    Lipopolysaccharides, from P. aeruginosa 10
  • HY-120538
    CPG-52364
    		Antagonist 98.49%
    CPG-52364 (compound 2) is a TLR9 antagonist. CPG-52364 inhibits the HEK293-hTLR9 cell with an IC50 value of 4.6 nM.
    CPG-52364
  • HY-13740G
    Resiquimod (GMP)
    		Agonist
    Resiquimod (R848) (GMP) is Resiquimod (HY-13740) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist. Resiquimod (GMP) can induce human mMDSC to mature into inflammatory macrophages.
    Resiquimod (GMP)
  • HY-118250
    GSK2245035
    		Agonist 99.79%
    GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for asthma.
    GSK2245035
  • HY-111269
    AZD8848
    		Agonist 99.14%
    AZD8848 is a selective toll-like receptor 7 (TLR7) anteagent agonist which is developed for the research of asthma and allergic rhinitis.
    AZD8848
  • HY-131945
    CU-115
    		Antagonist 99.63%
    CU-115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU-115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells.
    CU-115
  • HY-137345
    DB-3-291
    		Inhibitor 99.08%
    DB-3-291 is potent and selective PROTAC CSK degrader, with a Kd of 1 nM (Pink: CSK ligand (HY-131669); Blue: E3 ligase ligand (HY-103597); Black: linker (HY-N2407)).
    DB-3-291
  • HY-112051
    CU-CPT9b
    		Antagonist 99.03%
    CU-CPT9b is a specific TLR8 antagonist, with an IC50 of 0.7 nM. CU-CPT9b shows high binding affinity towards TLR8 with a Kd of 21 nM.
    CU-CPT9b
  • HY-146195
    MAPK-IN-1
    		Inhibitor
    MAPK-IN-1 (Compound 2) is a MAPK signaling pathway inhibitor. MAPK-IN-1 exhibits AChE inhibitory activity with an IC50 of 23.84 μM. MAPK-IN-1 shows anti-neuroinflammatory and neuroprotective activity and can be used for Alzheimer's disease research.
    MAPK-IN-1
  • HY-B0380
    Trimebutine
    		Inhibitor 99.42%
    Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
    Trimebutine
  • HY-B0180B
    Imiquimod maleate
    		Agonist 99.92%
    Imiquimod maleate (R 837 maleate), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod maleate exhibits antiviral and antitumor effects in vivo. Imiquimod maleate can be used for the research of external genital, perianal warts, cancer and COVID-19.
    Imiquimod maleate
  • HY-111358
    TLR7 agonist 1
    		Agonist 98.19%
    TLR7 agonist 1 is a potent, selective and oral TLR7 agonist with an IC50 of 90 nM.
    TLR7 agonist 1
  • HY-128799A
    CL097 hydrochloride
    		Agonist 99.96%
    CL097, a potent TLR7 and TLR8 agonist, induces pro-inflammatory cytokines in macrophages. CL097 induces NADPH oxidase priming, resulting in an increase of the fMLF-stimulated ROS production.
    CL097 hydrochloride
  • HY-120149
    Inotodiol
    		Inhibitor 98.29%
    Inotodiol activates p53 signaling pathway, inhibits MMP-2/9, and exhibits antitumor activity in cancer cell HeLa. Inotodiol inhibits the generation of ROS and exhibits antioxidant and neuroprotective effects. Inotodiol inhibits the activation of MAPK and NF-κB signaling pathway, and exhibits anti-inflammatory activity. Inotodiol inhibits TLR-4 mediated TNF-α production (IC50s in BMMC and BMDM is 0.7 μM and 3.0 μM), inhibits the degranulation in mast cell, exhibits anti-allergic activity. Inotodiol is orally active.
    Inotodiol
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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