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-162163
    TLR7 agonist 19
    Agonist
    TLR7 agonist 19 (Compound 14) is a Toll-like receptor 7 (TLR7) agonist with excellent pharmacokinetic properties and synergistic antitumor activity.
    TLR7 agonist 19
  • HY-153839
    ODN 4084-F
    ODN 4084-F is a class B (‘broadly-active’) inhibitory ODN. ODN 4084-F is potent inhibitor of TLR9-induced B cells and macrophages.
    ODN 4084-F
  • HY-18325A
    AN-3485 hydrochloride
    Inhibitor
    AN-3485 hydrochloride is a benzoxaborole analogue and an orally active antagonist of the Toll-like pathway. AN-3485 hydrochloride can inhibit TLR-mediated inflammatory cytokine secretion and has significant anti-inflammatory activity. In addition, AN-3485 hydrochloride also has certain anti-tumor activity.
    AN-3485 hydrochloride
  • HY-176837
    NOD2/TLR4 agonist-1
    Agonist
    NOD2/TLR4 agonist-1 (Compound 2) is a NOD2/TLR4 dual agonist. NOD2/TLR4 agonist-1 lacks immunostimulatory activity and serves as an important negative control in research.
    NOD2/TLR4 agonist-1
  • HY-P11014
    SjDX5-53 control peptide
    Control
    SjDX5-53 control peptide is a control peptide of the TLR2 activator SjDX5-53 (HY-P10982) that does not target a specific receptor and does not modulate regulatory T cells (Tregs) or dendritic cells. SjDX5-53 control peptide can be used to exclude nonspecific effects and help verify the specific role of SjDX5-53 in inducing Tregs and alleviating autoimmune diseases. SjDX5-53 control peptide is used in the study of autoimmune diseases such as colitis and psoriasis.
    SjDX5-53 control peptide
  • HY-N0201R
    Atractylenolide I (Standard)
    Antagonist
    Atractylenolide I (Standard) is the analytical standard of Atractylenolide I. This product is intended for research and analytical applications. Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
    Atractylenolide I (Standard)
  • HY-153838
    ODN 5328
    ODN 5328 (ODN 2395 Control) can be used as a sequence control for C-class ODN 2395. ODN 5328 shares the sequence with ODN 2395 but contain GpC dinucleotides instead of the CpG motifs.
    ODN 5328
  • HY-160227
    ORN 06
    Activator
    ORN 06 (Compound R-0006), a U-rich single-stranded RNA (containing 6 repeats of the UUG sequence motif), is a TLR7/8 agonist. ORN 06 stimulates human TLR7/8-mediated or murine TLR7-mediated immunity.
    ORN 06
  • HY-RS14587
    Tlr4 Mouse Pre-designed siRNA Set A
    Inhibitor

    Tlr4 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Tlr4 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Tlr4 Mouse Pre-designed siRNA Set A
  • HY-P991399
    CNTO-3157
    Inhibitor
    CNTO-3157 is a human IgG4 monoclonal antibody (mAb) targeting TLR3/CD283. CNTO-3157 can be used in Asthma and Ulcerative colitis research.
    CNTO-3157
  • HY-150726A
    Biotin-labeled ODN 1668 sodium
    Biotin-labeled ODN 1668 (sodium), a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. Biotin-labeled ODN 1668 (sodium) can be used to evaluate CpG ODN cellular uptake and localization using a biotin detection system and light microscopy.
    Biotin-labeled ODN 1668 sodium
  • HY-P991398
    IPH33
    Inhibitor
    IPH33 is a human monoclonal antibody (mAb) targeting TLR3/CD283. IPH33 can be used in Cancer and Inflammation research.
    IPH33
  • HY-158058
    WYJ-2
    Agonist
    WYJ-2 is a selective agonist for toll-like receptor 2/1 (TLR2/1) with EC50 of 18.57 nM in human TLR2 and TLR1 transient-cotransfected HEK 293T cells. WYJ-2 induces pyroptosis and exhibits anticancer activity against non-small cell lung cancer (NSCLC).
    WYJ-2
  • 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-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
Cat. No. Product Name / Synonyms Species Source
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