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-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-177665A
    Sitmutolimod sodium
    Agonist
    Sitmutolimod sodium, a CpG oligonucleotide, is a Toll-like receptor agonist with antineoplastic activity.
    Sitmutolimod sodium
  • 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
  • HY-145255
    Tri(TLR4-IN-C34-C2-amide-C3-amide-PEG1)-amide-C3-COOH
    Inhibitor
    Tri(TLR4-IN-C34-C2-amide-C3-amide-PEG1)-amide-C3-COOH 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.
    Tri(TLR4-IN-C34-C2-amide-C3-amide-PEG1)-amide-C3-COOH
  • HY-P1181
    Pam2CSK4
    Agonist
    Pam2CSK4 is a TLR2 agonist. Pam2CSK4 induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis.
    Pam2CSK4
  • HY-D1056B1
    Lipopolysaccharides, from Proteus vulgaris
    Lipopolysaccharides, from Proteus vulgaris are lipopolysaccharide endotoxins and TLR-4 activators derived from Proteus vulgaris, classified as S-type LPS, which can activate pathogen-associated molecular patterns (PAMP) of the immune system and induce cellular secretion of migrasomes. Lipopolysaccharides, from Proteus vulgaris exhibit a typical three-part structure: O-antigen, core oligosaccharide, and lipid A. Lipopolysaccharides, from Proteus vulgaris possess a unique molecular structure and chitosan affinity (Kb=2.72 μM), surpassing that of Yersinia pseudotuberculosis (Kb=6.06 μM) and Escherichia coli (Kb=79.50 μM).
    It is recommended to prepare a solution with concentration ≥2 mg/mL. Vortex thoroughly for more than 10 minutes. Due to the adsorption characteristics of LPS, silanized container or low adsorption centrifuge tubes should be used for aliquoting and storage, and mix thoroughly before use.
    Lipopolysaccharides, from Proteus vulgaris
  • HY-103639
    M62812 free base
    Inhibitor
    M62812 (free base) is a toll-like receptor 4 (TLR4) signal transduction inhibitor. M62812 can suppress endothelial cell and leukocyte activation and prevents lethal septic shock in mice. M62812 can be used for the research of sepsis.
    M62812 free base
  • HY-159672A
    3D-Monophosphoryl Lipid (12,16) free acid
    Agonist
    3D-Monophosphoryl Lipid (12,16) (3D-MPL (12,16)) free acid is a TLR4 agonist that can be used as a vaccine adjuvant to enhance the immunogenicity of vaccines.
    3D-Monophosphoryl Lipid (12,16) free acid
  • HY-168207
    TH023
    Inhibitor
    TH023 is an inhibitor for the TLR4 signaling pathway, that targets especially the formation of TLR4 homodimer. TH023 inhibits secreted embryonic alkaline phosphatase in cell HEK-Blue hTLR4 with an IC50 of 0.354 μM, and inhibits the NO expression in RAW264.7 with an IC50 of 1.61μM. TH023 also inhibits the activation of NF-κB, reduces the nuclear translocation of NF-κB p65. TH023 exhibits anti-inflammatory efficacy in LPS (HY-D1056)-induced mouse acute sepsis model, and ameliorates the mouse lung injury.
    TH023
  • HY-146244B
    FITC-labeled agatolimod sodium
    Agonist
    FITC-labeled agatolimod (sodium), a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. FITC-labeled agatolimod (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 agatolimod sodium
  • HY-P992458
    SBT8230
    Agonist
    SBT8230 is an ASGR1-targeted TLR8 agonist and an ASGR1-TLR8 immune TAC conjugate. SBT8230 achieves liver enrichment via conjugation with an anti-ASGR1 antibody, activates myeloid cells and induces anti-HBV immune responses. SBT8230 is applicable to research on chronic hepatitis B infection. The corresponding isotype control is: Human lgG1 kappa,lsotype Control (HY-P99001).
    SBT8230
  • HY-173070
    TLR7 agonist 29
    Agonist
    TLR7 agonist 29 (Compound 1) is the agonist for TLR7 with an EC50 of 5.2 nM for human TLR7 (EC50 for mouse TLR7 is 48.2 nM). TLR7 agonist 29 activates bone marrow-derived macrophages (BMDMs), stimulates myeloid cells in the tumor microenvironment, promotes the expression of PD-L1, CD86 and IFN-α. TLR7 agonist 29 can be used as payload for synthesis of ADC.
    TLR7 agonist 29
  • HY-B1370E
    (R)-Hydroxychloroquine phosphate
    Control
    (R)-Hydroxychloroquine ((R)-HCQ) phosphate is a (R)-isomer of Hydroxychloroquine (HY-W031727). (R)-Hydroxychloroquine inhibits the insulin metabolizing enzyme of cytosolic fraction of liver homogenates in healthy and diabetic rats.
    (R)-Hydroxychloroquine phosphate
  • HY-159672
    3D-Monophosphoryl Lipid (12,16)
    Agonist
    3D-Monophosphoryl Lipid (12,16) (3D-MPL (12,16)) is a TLR4 agonist that can be used as a vaccine adjuvant to enhance the immunogenicity of vaccines.
    3D-Monophosphoryl Lipid (12,16)
  • HY-157961
    E-5531
    Inhibitor
    E-5531 is an endotoxin antagonist. E-5531 quickly becomes inactive after binding with HDL. E-5531 can block the Toll like receptor 4 (TLR4) signaling pathway. E-5531 can be used for the study of endotoxemia and septic shock.
    E-5531
  • HY-N2345R
    Procyanidin B3 (Standard)
    Inhibitor
    Procyanidin B3 (Standard) is the analytical standard of Procyanidin B3. This product is intended for research and analytical applications. Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis.
    Procyanidin B3 (Standard)
  • HY-150751B
    FITC-labeled ODN TTAGGG sodium
    Antagonist
    FITC-labeled ODN TTAGGG (sodium), a inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. FITC-labeled ODN TTAGGG (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 TTAGGG sodium
  • HY-169057
    BI1543673
    Inhibitor
    BI1543673 is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor. BI1543673 can reduce the inflammatory response stimulated by TLR4 and TLR7/8 in human lung tissue. BI1543673 can decrease inflammatory signaling in a mouse model of lung inflammation induced by LPS.
    BI1543673
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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