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-150726B
    FITC-labeled ODN 1668 sodium
    		Agonist
    FITC-labeled ODN 1668 (sodium), a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. FITC-labeled ODN 1668 (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 1668 sodium
  • HY-N3097R
    Pellitorine (Standard)
    		Inhibitor
    Pellitorine (Standard) is the analytical standard of Pellitorine (HY-N3097). Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin (HY-10448), thereby reducing pain signal transmission. Pellitorine improves cognitive dysfunction by upregulating the BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. Pellitorine exerts anti-inflammatory and anti-sepsis effects by inhibiting the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Pellitorine exerts its antithrombotic effect by prolonging the clotting time, inhibiting the activity of clotting factors and thrombin. Pellitorine inhibits lipid peroxidation and resists ferroptosis by upregulating GPX4 and DHODH. Pellitorine kills Aedes aegypti mosquito larvae by inhibiting V-type H⁺-ATPase and aquaporin 4 (AaAQP4). Pellitorine exhibits anti-cancer activity (e.g., leukemia and breast cancer) and has inhibitory effects on certain bacteria.
    Pellitorine (Standard)
  • HY-178166
    ETI41
    		Inhibitor
    ETI41 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.63 μM) and TLR9 (IC50 = 0.16 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI41 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI41 suppresses the expression of inflammation-associated genes and effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI41 can be used for autoimmune and inflammatory diseases research.
    ETI41
  • HY-W777545
    4-[(7-Chloro-4-quinolinyl)amino]-1-pentanol-d4
    4-[(7-Chloro-4-quinolinyl)amino]-1-pentanol-d4 is the deuterium labeled Hydroxychloroquine Impurity E (HY-131262). Hydroxychloroquine Impurity E is the impurity of Hydroxychloroquine. Hydroxychloroquine is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro.
    4-[(7-Chloro-4-quinolinyl)amino]-1-pentanol-d<sub>4</sub>
  • HY-142963
    TLR4/NF-κB/MAPK-IN-1
    TLR4/NF-κB/MAPK-IN-1 is a new type of antineuroinflammatory agent by suppressing TLR4/NF-kB/MAPK pathways.
    TLR4/NF-κB/MAPK-IN-1
  • HY-150741A
    Biotin-labeled ODN 2216 sodium
    Biotin-labeled ODN 2216 (sodium) is a human-specific TLR9 (toll-like receptor 9) ligand or agonist. Biotin-labeled ODN 2216 (sodium) can be used to evaluate CpG ODN cellular uptake and localization using a biotin detection system and light microscopy.
    Biotin-labeled ODN 2216 sodium
  • HY-174465
    TLR4L 10
    		Ligand
    TLR4L 10 is a TLR4 ligand. TLR4L 10 induces cells to produce IL-6. TLR4L 10 has immunostimulatory activity.
    TLR4L 10
  • HY-N8903
    Mumefural
    		Inhibitor
    Mumefural is a bioactive component of the processed fruit of Prunus mume Sieb. Mumefural inhibits platelet aggregation. Mumefural shows anti-thrombotic effects and ameliorates cognitive impairment.
    Mumefural
  • HY-162115
    TLR7 agonist 17
    		Agonist
    TLR7 agonist 17 (compound 20) is a potent TLR7 agonist with EC50 values of 12 nM and 17 nM for hTLR7 and mTLR7, respectively. TLR7 agonist 17 shows anticancer activity.
    TLR7 agonist 17
  • HY-150725B
    FITC-labeled ODN 1585 sodium
    FITC-labeled ODN 1585 (sodium) is a potent inducer of IFN and TNFα production. FITC-labeled ODN 1585 (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 1585 sodium
  • 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-178136
    MyD88-IN-3
    		Inhibitor
    MyD88-IN-3 is an orally active, selective MyD88 Inhibitor. MyD88-IN-3 specifically targets the TIR domain of MyD88 (KD = 28.5 μM), thereby preventing MyD88 self-polymerization and interaction with TLRs, which suppresses the activation of MAPK and NF-κB pathways. MyD88-IN-3 demonstrates significant anti-inflammatory efficacy and effectively mitigates ALI (Acute Lung Injury) symptoms in CLP (cecal ligation and puncture) and Lipopolysaccharides (HY-D1056) (LPS)-induced ALI models. MyD88-IN-3 can be used for the study of ALI.
    MyD88-IN-3
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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