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

Toll-like Receptor (TLR)

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-153900
    TLR8 agonist 6
    Agonist
    TLR8 agonist 6 (Compound A) is a TLR8 agonist, with an EC50 of 0.052 μM. TLR8 agonist 6 induces IL-12p40 production in human PBMC (EC50: 0.031 μM). TLR8 agonist 6 can be used in the research of virus resistance, infection resistance, autoimmunity, tumor, etc.
    TLR8 agonist 6
  • HY-101132A
    (Rac)-VB-201
    Inhibitor
    (Rac)-VB-201 is the racemate of VB-201, an oxidized phospholipid small molecule that inhibits CD14- and toll-like receptor 2-dependent innate cell activation and suppresses atherosclerosis.
    (Rac)-VB-201
  • 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-P11072
    IRF5-CPP5
    Inhibitor
    IRF5-CPP5 is a cytosolic peptide that selectively inhibits human IRF5 with IC50 values of 15.4 and 15.3 μM for recombinant S430D or wild-type (WT) IRF5 dimerization, respectively..
    IRF5-CPP5
  • 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-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).
    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
  • 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-159671A
    3D-Monophosphoryl Lipid (14) triethylamine
    Agonist
    3D-Monophosphoryl Lipid (14) (3D-Monophosphoryl Lipid (14)) triethylamine is a TLR4 agonist that can be used as a vaccine adjuvant to enhance the immunogenicity of vaccines.
    3D-Monophosphoryl Lipid (14) triethylamine
  • HY-128741R
    D-Allose (Standard)
    Inhibitor
    D-Allose (Standard) is the analytical standard of D-Allose (HY-128741). This product is intended for research and analytical applications. D-Allose exhibits antitumor activity against various cancer cells. D-Allose scavenges reactive oxygen species (ROS) and reduces oxidative stress damage. D-Allose exhibits anti-inflammatory and neuroprotective through inhibition of TLR4/PI3K/AKT signaling pathway. D-Allose exhibits antihypertensive, cryoprotective, and anti-osteoporotic activities.
    D-Allose (Standard)
  • HY-176783
    GNE-5152
    Inhibitor
    GNE-5152 is an orthosteric SARM1 base-exchange (BE) inhibitor. GNE-5152 sustainably activates SARM1 at subinhibitory concentrations under mildly activating conditions, and this synergistic adverse effect increases NAD consumption, induces axon degradation and neurodegeneration and releases neurofilament-light (NfL) in cortical neurons. GNE-5152 can be used for neurodegenerative diseases research.
    GNE-5152
  • 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-159672B
    3D-Monophosphoryl Lipid (12,16) triethylamine
    Agonist
    3D-Monophosphoryl Lipid (12,16) (3D-MPL (12,16)) triethylamine is a TLR4 agonist that can be used as a vaccine adjuvant to enhance the immunogenicity of vaccines.
    3D-Monophosphoryl Lipid (12,16) triethylamine
  • 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-176487
    SARM1-IN-6
    SARM1-IN-6 (Compound 22b) is a brain-permeable SARM1 orthosteric inhibitor, the IC50 of SARM1-IN-6 against NAM is 0.069 μM.
    SARM1-IN-6
Cat. No. Product Name / Synonyms Species Source
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