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-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-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-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-B0180C
    Imiquimod dihydrochloride
    		Agonist
    Imiquimod (R 837) dihydrochloride, an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19.
    Imiquimod dihydrochloride
  • 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-181765
    TLR4/NF-κB-IN-2
    		Inhibitor
    TLR4/NF-κB-IN-2 is an orally active TLR4/NF-κB inhibitor and Nrf2/HO-1 activator. TLR4/NF-κB-IN-2 combats oxidative stress and exerts anti-inflammatory effects by regulating the Nrf2/HO-1 and TLR4/NF-κB pathways. TLR4/NF-κB-IN-2 reduces Aβ aggregation and protects neurons. TLR4/NF-κB-IN-2 can be used in the research of Alzheimer's disease.
    TLR4/NF-κB-IN-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-P5762A
    Phoenixin-14 TFA
    		Inhibitor
    Phoenixin-14 (PNX-14) TFA is an endogenous neuropeptide with multiple biological activities, and serves as the endogenous ligand of GPR173. Phoenixin-14 TFA reduces ROS production by inhibiting the HMGB1/TLR4/MyD88/NF-κB signaling axis, thereby exerting antioxidant and mitochondrial protective effects. Phoenixin-14 TFA inhibits FOXO3 phosphorylation by upregulating SIRT3 expression, suppresses apoptosis, and improves myocardial systolic/diastolic function. Phoenixin-14 TFA resists ferroptosis by activating the ATF4/SLC7A11/GPX4 axis; it activates ERK1/2 phosphorylation via GPR173. Phoenixin-14 TFA can be used in researches on neuroprotection, diabetes, cardiomyopathy, reproductive protection and so on.
    Phoenixin-14 TFA
  • 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-NP187
    Phytolacca americana Lectin
    Phytolacca americana Lectin (PWM) is an acidic monomeric glycoprotein specific to N-acetylglucosamine and a B cell-specific stimulator. Phytolacca americana Lectin acts as a mitogen to induce cell mitosis. Phytolacca americana Lectin sensitizes B cells to Toll-like receptor stimulation, enabling their activation by immunostimulatory DNA. When used in combination with copurified microbial Toll-like receptor ligands, Phytolacca americana Lectin triggers B cell proliferation and immunoglobulin secretion.
    Phytolacca americana Lectin
  • HY-183301
    TLR2/1 agonist-1
    		Agonist
    TLR2/1 agonist-1 is a selective agonist of the TLR2/1 heterodimer. TLR2/1 agonist-1 acts as a hematopoietic recovery inducer to accelerate the recovery of peripheral blood cells. TLR2/1 agonist-1 serves as a G-CSF production inducer to increase serum G-CSF levels. TLR2/1 agonist-1 exhibits radioprotective effects in mice exposed to radiation. TLR2/1 agonist-1 can be used in studies related to acute radiation syndrome.
    TLR2/1 agonist-1
  • HY-181916
    BXY-14
    		Agonist
    BXY-14 is a TLR2 agonist and vaccine adjuvant. BXY-14 significantly downregulates the expression of intratumoral PD-L1 in mouse models. BXY-14 acts as a vaccine adjuvant to induce antibody responses. BXY-14 exhibits synergistic efficacy when combined with the anti-PD-L1 monoclonal antibody Atezolizumab (HY-P9904) in mouse models of melanoma, and prolongs overall survival. BXY-14 is applicable to research related to melanoma.
    BXY-14
  • 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-124995
    BMS-986126
    		Inhibitor
    BMS-986126 is a potent, selective, and orally active IRAK4 inhibitor (IC50 = 5.3 nM). BMS-986126 broadly inhibits MyD88-dependent signaling pathways. BMS-986126 demonstrates robust activity in the MRL/lpr and NZB/NZW murine models of lupus, inhibiting multiple pathogenic responses. BMS-986126 can be used for autoimmune diseases research, such as lupus erythematosus (SLE).
    BMS-986126
  • 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>
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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