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-W782032B
    3D-Monophosphoryl Lipid A-5 triethylamine
    		Agonist
    3D-Monophosphoryl Lipid A-5 (3D-MPLA-5) triethylamine is a TLR agonist that can be used as an adjuvant for vaccines to enhance their immunogenicity.
    3D-Monophosphoryl Lipid A-5 triethylamine
  • HY-175293
    SMU-C68
    		Agonist
    SMU-C68 is a highly selective small-molecule TLR1/2 heterodimer agonist (EC50=0.009 μM). SMU-C68 activates NF-κB and MAPK pathways to promote pro-inflammatory cytokine release (e.g., TNF-α, IL-1β). SMU-C68 is promising for research of cancers.
    SMU-C68
  • HY-118250A
    GSK2245035 maleate
    		Agonist
    GSK2245035 maleate is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 maleate has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 maleate effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 maleate is used for asthma.
    GSK2245035 maleate
  • HY-159754
    HS201
    HS201 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.
    HS201
  • HY-178037
    TLR9 antagonist 1
    		Antagonist
    TLR9 antagonist 1 (Compound 38) is a selective TLR9 antagonist with an IC50 of 0.1  nM for hTLR9 over hTLR2/4/5/7/8. TLR9 antagonist 1 exacerbates disease symptoms with increased anti-dsDNA and anti-Sm levels in systemic lupus erythematosus (SLE) mouse models. TLR9 antagonist 1 can be used for inflammatory and immune diseases like lupus and arthritis research.
    TLR9 antagonist 1
  • HY-135811S1
    Desethyl chloroquine-d5
    		Inhibitor
    Desethyl chloroquine-d5 is deuterium labeled Desethyl chloroquine. 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-d<sub>5</sub>
  • HY-176553
    KBD4466
    		Inhibitor
    KBD4466 is an orally active potent TLR7 and TLR8 inhibitor with IC50s of 0.9 nM and 2.8 nM, respectively. KBD4466 inhibits the expression of inflammatory cytokines IL-6 and IFN-α. KBD4466 improves disease progression and survival in the BXSB/MpJ mouse model of Systemic Lupus Erythematosus (SLE). KBD4466 can be used in the study of autoimmune diseases.
    KBD4466
  • HY-153460
    TLR7/8/9 antagonist 2
    		Antagonist
    TLR7/8/9 antagonist 2 is an orally active TLR7/8/9 antagonist. TLR7/8/9 antagonist 2 has inhibitory activities for HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC50 values of 0.011 μM, 0.029 μM and 0,052 μM, respectively.TLR7/8/9 antagonist 2 has high bioavailability in vivo.TLR7/8/9 antagonist 2 can be used for the research of auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis.
    TLR7/8/9 antagonist 2
  • HY-150739
    ODN 21158
    		Inhibitor 98.16%
    ODN 21158 is a potent G-modified TLR3 and TLR9 inhibitor. ODN 21158 shows no cytotoxic. ODN 21158 inhibits IFN-α secretion in a dose dependent manner.
    ODN 21158
  • HY-175533
    TLR2 antagonist-1
    		Antagonist
    TLR2 antagonist-1 is a selective Toll-like receptor 2 (TLR2) antagonist. TLR2 antagonist-1 can effectively inhibit excessive TLR2 activation (IC50 = 11.41 μM) and the production of inflammatory factors. TLR2 antagonist-1 has metabolic stability with a half-life (T1/2) of 16.67 min in mouse liver microsomes. TLR2 antagonist-1 can be used for the researches of inflammation, immunology, and neurological disease.
    TLR2 antagonist-1
  • HY-RS14584
    Tlr3 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Tlr3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Tlr3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Tlr3 Mouse Pre-designed siRNA Set A
  • HY-159753
    HS105
    		Activator
    HS105 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.
    HS105
  • HY-173276
    SARM1-IN-4
    		Inhibitor
    SARM1-IN-4 (Compound 7) is an orally active SARM1 inhibitor. After being orally administered at a dose of 50 mg/kg in a mouse model, it can reduce the level of plasma neurofilament light chain (NfL). SARM1-IN-4 prevents programmed axonal degeneration by inhibiting the NAD+ hydrolase activity of SARM1, and it can be used in research related to neurodegenerative diseases and neurological disorders (such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, and peripheral neuropathies, etc.).
    SARM1-IN-4
  • HY-158694
    TLR7 agonist 20
    		Agonist
    TLR7 agonist 20 (compound 23) is an imidazoquinoline analogue. TLR7 agonist 20 is a potent TLR7 specific agonist, with an EC50 value of 0.23 μM for hTLR7. TLR7 agonist 20 shows strong adjuvant activity on spike antibody levels which induces a strong T helper 1 (Th1) response with increase in IgG2b and IgG2c, in addition to IgG1.
    TLR7 agonist 20
  • HY-163398
    TLR7-IN-1
    		Inhibitor
    TLR7-IN-1 (compound 16-A) is a TLR7 inhibitor with an EC50 value of 0.001 µM.
    TLR7-IN-1
  • HY-170899
    TLR7 agonist 28
    		Agonist
    TLR7 agonist 28 (compound 3) is a potent TLR7 agonist. TLR7 agonist 28 can conjugat to antitumor monoclonal antibodies (mAbs) for cancer immunotherapy.
    TLR7 agonist 28
  • HY-159670B
    Monophosphoryl Lipid A-12 triethylamine
    		Agonist
    Monophosphoryl Lipid A-12 (triethylamine) is a toll-like receptor 4 agonist. Monophosphoryl Lipid A-12 (triethylamine) can be used for the research of immunization and vaccine.
    Monophosphoryl Lipid A-12 triethylamine
  • HY-B1370S
    Hydroxychloroquine-d4 sulfate
    		Inhibitor
    Hydroxychloroquine-d4 (sulfate) is the deuterium labeled Hydroxychloroquine sulfate. Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro.
    Hydroxychloroquine-d<sub>4</sub> sulfate
  • HY-147310
    CU-CPD107
    		Agonist 98.07%
    CU-CPD107 is a potent, selective toll-like receptor 8 (TLR 8) agonist. CU-CPD107 inhibits TLR8 signaling. CU-CPD107 converts to synergistic agonist activities in the presence of ssRNA and induces TLR8 signaling. CU-CPD107 inhibits proinflammatory factor expression and avoids immune responses in the presence of ssRNA.
    CU-CPD107
  • HY-170489
    Antifungal agent 123
    		Inhibitor
    Antifungal agent 123 (Compound 4b) exhibits good affinity to the oxidoreductase of Staphylococcus aureus or the membrane protein of Candida albicans, exhibits antibacterial and antifungal activities. Antifungal agent 123 scavenges free radical, exhibits antioxidant efficacy. Antifungal agent 123 inhibits the TLR signaling pathway, and exhibits anti-inflammatory efficacy.
    Antifungal agent 123
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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