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-N0703R
    Schaftoside (Standard)
    		Inhibitor
    Schaftoside (Standard) is the analytical standard of Schaftoside. This product is intended for research and analytical applications. Schaftoside is a flavonoid found in a variety of Chinese herbal medicines, such as Eleusine indica. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission.
    Schaftoside (Standard)
  • HY-N12110
    SMU-CX1
    		Inhibitor
    SMU-CX1 is a specific TLR3 inhibitor (IC50: 0.11 μM) with IC50 ranging from 0.14-0.33 μM against multiple influenza A virus subtypes. SMU-CX1 inhibits the viral PB2 and NP proteins with an IC50 of 0.43 μM for SARS-CoV-2 activity. SMU-CX1 also inhibits inflammatory factors in host cells, including IFN-β, IP-10, and CCL-5.
    SMU-CX1
  • HY-150738A
    Biotin-labeled ODN 2088 sodium
    Biotin-labeled ODN 2088 (sodium) is a potent TLR3, TLR7 and TLR9 inhibitor. Biotin-labeled ODN 2088 (sodium) can be used to evaluate CpG ODN cellular uptake and localization using a biotin detection system and light microscopy.
    Biotin-labeled ODN 2088 sodium
  • HY-P2358A
    PSMα3 TFA
    		Inhibitor
    PSMα3 TFA is a peptide for manipulating DCs to become tolerogenic for DC vaccination strategies. PSMα3 TFA penetrates and modulates human monocyte-derived DCs by altering the TLR2- or TLR4-induced maturation, inhibiting pro- and anti-inflammatory cytokine production and reducing antigen uptake. PSMα3 TFA is an important toxin released by the most virulent strains of methicillin-resistant Staphylococcus aureus (MRSA).
    PSMα3 TFA
  • HY-135811
    Desethyl chloroquine
    		Inhibitor
    Desethyl chloroquine is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine possesses antiplasmodic activity.
    Desethyl chloroquine
  • HY-B0730R
    Pamidronate disodium pentahydrate (Standard)
    		Antagonist
    Pamidronate (disodium pentahydrate) (Standard) is the analytical standard of Pamidronate (disodium pentahydrate). This product is intended for research and analytical applications. Pamidronate disodium pentahydrate, the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronate disodium pentahydrate significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of osteoprotegerin in cartilage and subchondral bone, and inhibiting the expression of RANKL and MMP-9 in both tissues, as well as TLR-4 in cartilage, thereby alleviating cartilage degeneration. Additionally, Pamidronate disodium pentahydrate can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma.
    Pamidronate disodium pentahydrate (Standard)
  • HY-P10586
    Macrophage-activating lipopeptide 2
    		Activator
    Macrophage-activating lipopeptide 2 (MALP-2) is an agonist of Toll like receptors TLR-2/TLR-6. Macrophage-activating lipopeptide-2 can enhance endothelial nitric oxide synthase (eNOS) phosphorylation and endothelial cell release of NO, thereby improving vasodilation. Macrophage-activating lipopeptide-2 can enhance 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
  • HY-D1056C5
    Lipopolysaccharides, from S. enterica serotype minnesota Re 595 (Re mutant)
    		Ligand
    Lipopolysaccharides (LPS), from S. enterica (Salmonella enterica) serotype minnesota Re 595 (Re mutant) is prepared from Salmonella enterica strain Re 595 (Re mutant). The structure in the LPS of strain Re 595 was shown to induce secretion and aggregation in human platelets.
    Lipopolysaccharides, from S. enterica serotype minnesota Re 595 (Re mutant)
  • HY-17589S
    Chloroquine-d5 diphosphate
    		Inhibitor
    Chloroquine-d5 (diphosphate) is the deuterium labeled Chloroquine (phosphate). Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
    Chloroquine-d<sub>5</sub> diphosphate
  • HY-RS14576
    TLR1 Human Pre-designed siRNA Set A
    		Inhibitor

    TLR1 Human Pre-designed siRNA Set A contains three designed siRNAs for TLR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    TLR1 Human Pre-designed siRNA Set A
    TLR1 Human Pre-designed siRNA Set A
  • HY-150215A
    ODN 105870 sodium
    		Inhibitor
    ODN 105870 sodium, a G-modified inhibitory oligonucleotide (INH-ODN), is a selective TLR7 inhibitor. ODN 105870 sodium can be uesd for inflammatory immune responses research.
    ODN 105870 sodium
  • HY-161630
    TLR8 agonist 8
    		Agonist
    TLR8 agonist 8 (Compound II-72) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 8 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 8 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 89%.
    TLR8 agonist 8
  • HY-D1056B2
    Lipopolysaccharides, from Proteus mirabilis
    Lipopolysaccharides, from Proteus mirabilis are lipopolysaccharide endotoxins and TLR-4 activators derived from Proteus mirabilis, 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 Proteus mirabilis exhibit a typical three-part structure: O-antigen, core oligosaccharide, and lipid A. Proteus mirabilis is a major pathogen causing urinary tract infections and may also contribute to rheumatoid arthritis. Lipopolysaccharides, from Proteus mirabilis also exhibit potential anti-tumor effects, demonstrating in vivo inhibitory activity against solid tumors such as meningosarcoma and Walker carcinosarcoma.
    Lipopolysaccharides, from Proteus mirabilis
  • HY-153839A
    ODN 4084-F sodium
    		Inhibitor
    ODN 4084-F sodium is a class B (‘broadly-active’) inhibitory ODN. ODN 4084-F sodium is potent inhibitor of TLR9-induced B cells and macrophages.
    ODN 4084-F sodium
  • HY-17007S
    Saquinavir-d9
    		Inhibitor
    Saquinavir-d9 (Ro 31-8959-d9) is the deuterium labeled Saquinavir (HY-17007). Saquinavir (Ro 31-8959) is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir also has anti-inflammatory activity and can induce apoptosis of human red blood cells.
    Saquinavir-d<sub>9</sub>
  • HY-145253
    Tri(TLR4-IN-C34-C2-amide-PEG1)-amide-C3-COOH
    		Inhibitor
    Tri(TLR4-IN-C34-C2-amide-PEG1)-amide-C3-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.
    Tri(TLR4-IN-C34-C2-amide-PEG1)-amide-C3-COOH
  • HY-P10208
    RKH
    		Antagonist
    PKH is a TLR4 antagonist. PKH is a novel tripeptide and can be isolated from Akkermansia muciniphila. RKH reduces sepsis-induced inflammatory cell activation and proinflammatory factor overproduction.
    RKH
  • HY-139785A
    Cavrotolimod sodium
    		Inhibitor
    Cavrotolimod sodium is an immunostimulatory spherical nucleic acid (SNA) modified with type B CpG oligonucleotides designed to agonize TLR9 and elicit immune responses useful in oncology applications.
    Cavrotolimod sodium
  • HY-149650A
    TLR4 agonist-1 TEA
    		Agonist
    TLR4 agonist-1 (TEA) (compound 17a) is a potent agonist of Toll-like Receptor 4 (TLR4), and induces the generation of MIP-1β in RAW 264.7 and MM6 cells.
    TLR4 agonist-1 TEA
  • HY-144497
    HE-S2
    		Activator
    HE-S2 is an antibody-drug conjugate triggering a potent antitumor immune response. HE-S2 acts by blocking the PD-1/PD-L1 interaction and activating the Toll-like receptor 7/8 (TLR7/8) signaling pathway. HE-S2 has remarkable antitumor activity.
    HE-S2
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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