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-169242
    JAK1-IN-16
    Inhibitor
    JAK1-IN-16 (compound 4l) is an inhibitor of JAK1/STAT3 and effectively downregulates TLR4 protein expression..
    JAK1-IN-16
  • HY-P992348
    DS-7011a
    Inhibitor
    DS-7011a is a selective inhibitor targeting TLR7. DS-7011a inhibits IL-6 production induced by TLR7 stimulation and related responses in B cells and plasmacytoid dendritic cells. DS-7011a is internalized in a TLR7-dependent manner and accumulates in B cells, various dendritic cell subsets, and monocytes/macrophages. DS-7011a can be used in research related to systemic lupus erythematosus (SLE).
    DS-7011a
  • HY-177665
    Sitmutolimod
    Agonist
    Sitmutolimod, a CpG oligonucleotide, is a Toll-like receptor agonist with antineoplastic activity.
    Sitmutolimod
  • HY-153070
    TLR7 agonist 5
    Agonist
    TLR7 agonist 5 (compound IIb-11) is an TLR7 agonist with an EC50 value of ~4 nM.
    TLR7 agonist 5
  • HY-159751
    HS101
    Agonist
    HS101 is a vaccine adjuvant and a key component in vaccines. Adjuvants can be divided into immunostimulants and delivery systems. Adjuvants can not only enhance the intensity and durability of immune responses, but also affect the type of immune responses. On the one hand, immunostimulants promote the production of antigen signals and co-stimulatory signals by targeting Toll-like receptors (TLRs) and other pattern recognition receptors (PRRs), leading to the maturation and activation of antigen presenting cells (APCs), thereby enhancing adaptive immune responses; on the other hand, delivery systems are carrier materials that promote antigen delivery by prolonging the bioavailability of loaded antigens and targeting antigens to lymph nodes or APCs. Several common adjuvants include: saponins, TLRs agonists, polysaccharides, nanoparticles, cytokines, and mucosal adjuvants.
    HS101
  • HY-N6612A
    D-Glucuronic acid sodium salt monohydrate
    Agonist 98.0%
    D-Glucuronic acid sodium salt monohydrate is a major component of many anti-inflammatory proteoglycans, which can promote embryonic development and inhibit cell aggregation. After being metabolized into ethyl glucuronide (HY-113093), D-Glucuronic acid sodium salt monohydrate activates Toll-like receptor 4 (TLR4), causing pain. D-Glucuronic acid sodium salt monohydrate and its derivative glucurono-lactone can serve as liver detoxifiers, and its derivatives also possess anti-tumor activity.
    D-Glucuronic acid sodium salt monohydrate
  • HY-164386
    Defoslimod
    Agonist
    Defoslimod (OM 174) is an agonist for TLR4 receptor and acts as an immunomodulator. Defoslimod activates macrophages and dendritic cells, induces cytokines secretion, and exhibits antitumor efficacy in rats.
    Defoslimod
  • HY-N16013
    FP-18 disodium
    FP-18 disodium, a TLR-4 agonist, is a vaccine adjuvant.
    FP-18 disodium
  • HY-N6928R
    Mogroside III-E (Standard)
    Mogroside III-E (Standard) is the analytical standard of Mogroside III-E. This product is intended for research and analytical applications. Mogroside III-E is a cucurbitane-type compound isolated from Siraitia grosvenorii, inhibits NO release, with anti-fibrotic activity.
    Mogroside III-E (Standard)
  • HY-181796
    TLR7 antagonist-1
    Antagonist
    TLR7 antagonist-1 (Compound 44#) is an orally active, selective TLR7 antagonist with an IC50 value of 0.3 nM against TLR7. TLR7 antagonist-1 selectively binds to TLR7, inhibits its activation, and downregulates the c-Rel signaling pathway. TLR7 antagonist-1 downregulates the mRNA levels of proinflammatory cytokines IL-1β, IL-6, and TNF-α. TLR7 antagonist-1 alleviates Imiquimod (HY-B0180)-induced psoriasis-like skin lesions. TLR7 antagonist-1 is applicable to research related to psoriasis.
    TLR7 antagonist-1
  • HY-171239
    Ste2Cys
    Ligand
    Ste2Cys is a diacylglycerol cysteine-type immunologic adjuvant lipid molecule. Ste2Cys can bind to TLR2 and activate NF-κB signaling pathway. Ste2Cy can upregulate the expression of MHC II class molecules on the surface of mouse bone marrow-derived D1 dendritic cells. Ste2Cys can be used for research of the development of immunologic vaccines.
    Ste2Cys
  • HY-150751A
    Biotin-labeled ODN TTAGGG sodium
    Biotin-labeled ODN TTAGGG (sodium), a inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. Biotin-labeled ODN TTAGGG (sodium) can be used to evaluate CpG ODN cellular uptake and localization using a biotin detection system and light microscopy.
    Biotin-labeled ODN TTAGGG sodium
  • HY-150724A
    Biotin-labeled ODN 1018 sodium
    Biotin-labeled ODN 1018 (sodium), an oligodeoxynucleotide, is a TLR-9 agonist. Biotin-labeled ODN 1018 (sodium) can be used to evaluate CpG ODN cellular uptake and localization using a biotin detection system and light microscopy.
    Biotin-labeled ODN 1018 sodium
  • HY-150219
    ODN M326
    Agonist
    ODN M326 (CpG-ODN M326) is a potent TLR9 agonist. ODN M326 induces the production of TNF. ODN M326 can be used as a vaccine adjuvant.
    ODN M326
  • HY-P990519
    Anti-TLR3/CD283 Antibody (CNTO5429)
    Anti-TLR3/CD283 Antibody (CNTO5429) is a CHO expressed human antibody that targets TLR3/CD283. Anti-TLR3/CD283 Antibody (CNTO5429) has a huIgG2 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 145.42 kDa. The isotype control for Anti-TLR3/CD283 Antibody (CNTO5429) can be referenced as Human IgG4 kappa, Isotype Control (HY-P99003).
    Anti-TLR3/CD283 Antibody (CNTO5429)
  • HY-161631
    TLR8 agonist 9
    Agonist
    TLR8 agonist 9 (Compound II-77) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 9 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 9 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 97%.
    TLR8 agonist 9
  • HY-148555
    AXC-879
    Agonist
    AXC-879, a TLR agonist (EC50: 157.2 nM). AXC-879 is an ADC Cytotoxin and can be used for ADC synthesis.
    AXC-879
  • HY-P11232
    NAB815
    Inhibitor
    NAB815 is a specific inhibitor of the Stx2a (Kd = 0.01 μM)/TLR4 interaction. NAB815 inhibits the neutrophil/Stx2a interaction (IC50 = 0.057 μg/mL). NAB815 inhibits the formation of Stx2-containing extracellular vesicles (EVs) produced by leukocytes and platelets and reduces their toxic effects in cellular (Vero cells) and animal models (CD-1 mice). NAB815 reduces bacterial loads in the kidneys, urine, and bladders of Escherichia coli-infected mice. NAB815 is useful in the study of hemolytic uremic syndrome (HUS).
    NAB815
  • HY-159671B
    3D-Monophosphoryl Lipid (14) ammonium
    Agonist
    3D-Monophosphoryl Lipid (14) (3D-MPL (14)) ammonium is a TLR agonist that can be used as a vaccine adjuvant to enhance the immunogenicity of vaccines.
    3D-Monophosphoryl Lipid (14) ammonium
  • HY-162845
    TLR7/8 agonist 11
    Agonist
    TLR7/8 agonist 11 (compound 30) is a potent agonist of hTLR7 and hTLR8, with EC50s of 31.1 nM and 13.1 nM, respectively. TLR7/8 agonist 11 plays an important role in adaptive and innate immune responses.
    TLR7/8 agonist 11
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