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-153544
    TLR7/8 agonist 9
    Inhibitor
    TLR7/8 agonist 9 (Compound 25a) is a TLR7/8 agonist, with EC50s of 40 nM and 23 nM for hTLR7/8. TLR7/8 agonist 9 has anti-tumor activity and improves the antitumor activity of PD-1/PD-L1 blockade. TLR7/8 agonist 9 can be used for research of cancer immunotherapy.
    TLR7/8 agonist 9
  • HY-N6949R
    Juglone (Standard)
    Inhibitor
    Juglone (Standard) is the analytical standard of Juglone. This product is intended for research and analytical applications. Juglone (5-hydroxy-1,4-naphthalenedione) is a yellow dye that can be extracted from Juglans regia. Juglone induces apoptosis through the mitochondrial pathway. Juglone has antibacterial and antitumor activity .
    Juglone (Standard)
  • HY-161026
    JM-9
    Inhibitor
    JM-9 is a inhibitor of MD2. JM-9 suppresses high glucose and palmitic acid -induced inflammation in MPMs. JM-9 improves diabetic kidney disease by inhibiting MD2-mediated inflammation.
    JM-9
  • HY-162116
    TLR7 agonist 18
    Agonist
    TLR7 agonist 18 (Compound 21a) is a selective Toll-like receptor 7 (TLR7) agonist with an EC50 of 7.8 μM. TLR7 agonist 18 is not cytotoxic to hTLR7 cotransfected HEK293 cell lines and can induce the secretion of several cytokines, including IL-1β, IL-12p70, IL-8, and TNF-α. TLR7 agonist 18 can be used in vaccine, asthma, allergy and anti-cancer research.
    TLR7 agonist 18
  • HY-B0012AR
    Pamidronate (disodium) (Standard)
    Inhibitor
    Pamidronate disodium (Standard) is the analytical standard of Pamidronate disodium.Pamidronate disodium (Standard), the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronate disodium (Standard) significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of OPG 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 (Standard) can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma.
    Pamidronate (disodium) (Standard)
  • HY-150739A
    ODN 21158 sodium
    Inhibitor
    ODN 21158 sodium is a potent G-modified TLR3 and TLR9 inhibitor. ODN 21158 sodium inhibits IFN-α secretion in a dose dependent manner.
    ODN 21158 sodium
  • HY-145254
    Tri(TLR4-IN-C34-PEG2-amide-PEG1)-amide-C3-COOH
    Inhibitor
    Tri(TLR4-IN-C34-PEG2-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-PEG2-amide-PEG1)-amide-C3-COOH
  • HY-150738B
    FITC-labeled ODN 2088 sodium
    Antagonist
    FITC-labeled ODN 2088 (sodium) is a potent TLR3, TLR7 and TLR9 inhibitor. FITC-labeled ODN 2088 (sodium) can be used to evaluate CpG ODN cellular uptake and localization by confocal laser-scanning microscopy (excitation 495 nm, emission 520 nm) or flow cytometry.
    FITC-labeled ODN 2088 sodium
  • HY-145886
    TLR7/8 antagonist 1
    Antagonist
    TLR7/8 Antagonist 1 (Compound 16c) is the potent antagonist of TLR7/8 with IC50s of 3.91 and 2.19 μM, respectively. TLR7/8 Antagonist 1 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for researching infectious disease, cancer, and autoimmune disorders.
    TLR7/8 antagonist 1
  • HY-160040
    Cobitolimod
    Agonist
    Cobitolimod is a DNA oligonucleotide agonist of TLR-9 with anti-inflammatory activity. Cobitolimod suppresses Th17 cells and induces anti-inflammatory FoxP3 and IL-10 expression, inhibiting the IL-17 signaling pathway.
    Cobitolimod
  • HY-168157
    TLR7 agonist 26
    Agonist
    TLR7 agonist 26 (Compound 4) is a potent Toll-like receptor 7 (TLR7) agonist, with an EC50 of 225.5 nM. TLR7 agonist 26 shows immunopotentiating effects.
    TLR7 agonist 26
  • HY-P2848A
    Cholesterol oxidase, rhodococcus sp
    Inhibitor
    Cholesterol oxidase, Rhodococcus sp. is a key enzyme in the cholesterol degradation process. It catalyzes the isomerization and oxidation of cholesterol mediated by the coenzyme FAD. Research indicates that cholesterol oxidase plays a crucial role in the pathogenicity of Mycobacterium tuberculosis by modulating the host macrophage immune response through inhibition of the Toll-like receptor 2 (TLR2) signaling pathway, thereby enhancing the survival of Mycobacterium tuberculosis. Cholesterol oxidase, from Rhodococcus sp., shows potential for research in the field of tuberculosis.
    Cholesterol oxidase, rhodococcus sp
  • HY-130320A
    Monophosphoryl lipid A free acid
    Agonist
    Monophosphoryl lipid A (free acid) is a toll-like receptor 4 agonist. Monophosphoryl lipid A (free acid) is derived from the cell wall of nonpathogenic Salmonella. Monophosphoryl lipid A (free acid) can be used for the research of immunization and vaccine.
    Monophosphoryl lipid A free acid
  • HY-156175
    TLR7 agonist 14
    Agonist
    TLR7 agonist 14 (compound 17b) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 14 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations.
    TLR7 agonist 14
  • HY-B0180S1
    Imiquimod-d9
    Agonist
    Imiquimod-d9 is deuterium labeled Imiquimod. Imiquimod (R 837), 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[1][2].
    Imiquimod-d<sub>9</sub>
  • HY-B0180S
    Imiquimod-d6
    Agonist
    Imiquimod-d6 is the deuterium labeled Imiquimod. Imiquimod (R 837), 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[1][2].
    Imiquimod-d<sub>6</sub>
  • HY-159919
    UM-3006
    Agonist
    UM-3006 is a highly efficient TLR7/8 agonist that enhances immune responses by activating the TLR signaling pathway. UM-3006 holds significant research and application potential in the fields of vaccine adjuvants and immune diseases.
    UM-3006
  • HY-W008341
    5-Chloroisoquinoline
    Inhibitor
    5-Chloroisoquinoline (compound 42) is an inhibitor of SARM1 (Sterile alpha and toll/interleukin receptor (TIR) motif containing protein 1), an enzyme involved in axon degeneration that catalyzes multiple activities through a ternary complex mechanism. 5-Chloroisoquinoline can be used in the study of neurodegenerative diseases or axon degeneration.
    5-Chloroisoquinoline
  • HY-164485
    INI-4001
    Activator
    INI-4001 is a TLR7/8 agonist, with EC50 values of 1.89 μM and 4.86 μM for TLR7/8, respectively. INI-4001 induces signaling and SEAP production through TLR7 and TLR8. INI-4001 promotes the generation of high-affinity, specific antibodies against fentanyl, preventing fentanyl from crossing the blood-brain barrier, making it an effective adjuvant for fentanyl vaccines in the opioid use disorder (OUD) population.
    INI-4001
  • HY-N0022R
    Isoacteoside (Standard)
    Inhibitor
    Isoacteoside (Standard) is the analytical standard of Isoacteoside. This product is intended for research and analytical applications. Isoacteoside is a natural product that can significantly inhibit the formation of glycation end products.
    Isoacteoside (Standard)
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