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-153840B
    ODN INH 18 triethylamine
    99.59%
    ODN INH-18 triethylamine is a linear 24-mer class B INH-ODN in which the 5' INH-ODN 4084-F sequence was followed by a random stretch of 12 nucleotides lacking the ability to form significant secondary structures. ODN INH-18 triethylamine showes inhibitory potency for TLR9 ligand-induced IFN-α production.
    ODN INH 18 triethylamine
  • HY-164485
    INI-4001
    Activator
    INI-4001 is a TLR7/8 agonist and vaccine adjuvant. INI-4001 regulates innate and adaptive immune responses by activating murine TLR7 and human TLR7/TLR8. INI-4001 enhances IgG and neutralizing antibody responses against Powassan virus (POWV), reduces viral loads in the brain, liver and spleen, provides complete protection against lethal POWV challenge, and skews immune responses toward a Th1 phenotype. When INI-4001 is used in combination with Al (OH)3 and SARS-CoV-2 RBD antigen, it efficiently adsorbs to Al (OH)3, promotes Th1 immunity and enhances SARS-CoV-2 neutralizing antibody responses. INI-4001 is applicable to research related to Powassan virus infection and COVID-19.
    INI-4001
  • HY-P9994
    Pertuzumab zuvotolimod
    Agonist 98.64%
    Pertuzumab zuvotolimod (SBT6050) is an anti-HER2 antibody-drug conjugate (ADC). Pertuzumab zuvotolimod is composed of a humanized anti-HER2 antibody (Pertuzumab) (HY-P9912A), a linker, a TLR8 agonist payload, and the drug-linker conjugate for ADC is Zuvotolimod (HY-145620). Pertuzumab zuvotolimod potently induces multiple anti-tumor immune activities through the direct activation myeloid cells and the subsequent induction of T and NK cell cytolytic activity. Pertuzumab zuvotolimod can be used for HER2-expressing solid tumors research.
    Pertuzumab zuvotolimod
  • HY-139575A
    Guretolimod hydrochloride
    98.67%
    Guretolimod hydrochloride is a Toll-like receptor 7 (TLR7) agonist.
    Guretolimod hydrochloride
  • HY-145961
    TLR7 agonist 4
    Agonist 98.87%
    TLR7 agonist 4 is a TLR7 agonist with pro-inflammatory cytokine-stimulating activity. TLR7 agonist 4 modulates TLR7 activity to stimulate the production of pro-inflammatory cytokines. TLR7 agonist 4 stimulates mouse bone marrow-derived macrophages to produce the pro-inflammatory cytokine TNFα. TLR7 agonist 4 can be conjugated with antibodies to form conjugates. TLR7 agonist 4 is applicable to cancer research.
    TLR7 agonist 4
  • HY-W031727S
    Hydroxychloroquine-d4-1 sulfate
    Inhibitor ≥98.0%
    Hydroxychloroquine-d4-1 (sulfate) is the deuterium labeled 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.
    Hydroxychloroquine-d<sub>4</sub>-1 sulfate
  • HY-RS14599
    TLR9 Human Pre-designed siRNA Set A
    Inhibitor

    TLR9 Human Pre-designed siRNA Set A contains three designed siRNAs for TLR9 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    TLR9 Human Pre-designed siRNA Set A
  • HY-145960
    MC-Val-Cit-PAB-Amide-TLR7 agonist 4
    Agonist 99.39%
    MC-Val-Cit-PAB-Amide-TLR7 agonist 4 (example 15) is a HER2-TLR7 and HER2-TLR8 immune agonist conjugate.
    MC-Val-Cit-PAB-Amide-TLR7 agonist 4
  • HY-161918
    SARM1-IN-3
    Inhibitor
    SARM1-IN-3 (Example 30) is a SARM1 inhibitor. SARM1-IN-3 can be used in the study of chemotherapy induced peripheral neuropathy (CIPN).
    SARM1-IN-3
  • HY-145245
    TLR4-IN-C34-C2-amide-C6-OH
    Inhibitor 99.62%
    TLR4-IN-C34-C2-amide-C6-OH 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.
    TLR4-IN-C34-C2-amide-C6-OH
  • HY-P10897
    SjDX5-271
    Inhibitor 98.90%
    SjDX5-271 is a small 3 kDa peptide. SjDX5-271 inhibits the TLR4/MyD88/NF-κB signaling pathway. SjDX5-271 induces cell polarization. SjDX5-271 alleviats hepatic inflammation. SjDX5-271 protects mice against liver ischemia-reperfusion injury.
    SjDX5-271
  • HY-150745
    ODN 24987
    Inhibitor
    ODN 24987 is a Guanine-modified inhibitory oligonucleotides (ODN), targeting TLR9. ODN 24987 can inhibit IL-6 and IFN-α release. ODN 24987 can be used for research immune disorders. ODN 24987 sequence: 5’-C-C-T-G-G-C-c7G-G-G-G-3’.
    ODN 24987
  • HY-N11768
    4-Methoxylonchocarpin
    Inhibitor 98.0%
    4-Methoxylonchocarpin is an orally active anti-inflammatory agent. 4-methoxylonchocarpin inhibits the binding of LPS to Toll-like Receptor (TLR) TLR4 to inhibit NF-κB activation and TNF Receptor and IL-6 expression. 4-Methoxylonchocarpin also inhibits the phosphorylation of TGF-beta activated kinase 1 and TNBS-induced expression of IL-1β, IL-17A, and TNF. 4-methoxylonchocarpin can improve 2,4, 6-trinitrobenzene sulfonic acid (TNBS)-induced colitis mouse model.
    4-Methoxylonchocarpin
  • 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-105070A
    Eritoran tetrasodium
    Antagonist
    Eritoran tetrasodium (E5564) is a Toll-like receptor 4 (TLR4) antagonist. Eritoran tetrasodium protects mice against lethal influenza virus infection, such as Ebola virus (EBOV), Marburg virus (MARV). Eritoran tetrasodium decreases the level of granulocytosis, may alleviate the severity of the "cytokine storm". Eritoran tetrasodium inhibits pathogenesis of filovirus infection. Eritoran tetrasodium has anti-inflammatory activity.
    Eritoran tetrasodium
  • HY-P5642A
    Retrocyclin-101 TFA
    Inhibitor
    Retrocyclin-101 (RC-101) TFA is an artificially synthesized, cyclic-structured θ-defensin, a broad-spectrum agent with antimicrobial (covering viruses, bacteria, and fungi) activity and anti-inflammatory activity. Retrocyclin-101 TFA can inhibit the serine protease activity of ZIKV NS2B-NS3, with an IC50 of 7.20 μM. Retrocyclin-101 TFA has significant inhibitory activity against HIV, SARS-CoV-2, flaviviruses, influenza viruses, HSV-1/2, Staphylococcus aureus, etc. Retrocyclin-101 TFA inhibits the signal transduction mediated by TLR4 and TLR2, reducing the expression of pro-inflammatory cytokines.
    Retrocyclin-101 TFA
  • 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-178037
    TLR9 antagonist 1
    Antagonist
    TLR9 antagonist 1 is a selective hTLR9 antagonist with an IC50 of 0.1 nM against hTLR9. TLR9 antagonist 1 exhibits favorable pharmacokinetic and pharmacodynamic properties. TLR9 antagonist 1 can be used in the research of systemic lupus erythematosus.
    TLR9 antagonist 1
  • 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-P5117
    TAT-CIRP
    Inhibitor 98.32%
    TAT-CIRP is a a small peptide, refers to Trans-trans-activating (Tat)-cold-inducible RNA binding protein. TAT-CIRP is an inhibitor of myeloid differentiation protein 2 (MD2). TAT-CIRP exhibits robust neuroprotection against ischemic and hemorrhagic stroke in mice.
    TAT-CIRP
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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