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-153841
    ODN INH-1
    ODN INH-1 is palindromic and a class R (‘restricted’) inhibitory ODN. ODN INH-1 is a potent inhibitor of TLR9-induced B cells and macrophages
    ODN INH-1
  • HY-162004
    NF-κB-IN-14
    		Inhibitor
    NF-κB-IN-14 (compound 5e) significantly inhibits nitric oxide production in LPS-induced macrophages (IC50: 6.4 μM). NF-κB-IN-14 disrupts the TLR4-MyD88 protein interaction, leading to the suppression of the NF-κB signaling pathway suppression. NF-κB-IN-14 reduces ear edema and inflammation in an atopic dermatitis mouse model.
    NF-κB-IN-14
  • HY-150216A
    ODN 105871 sodium
    		Inhibitor
    ODN 105871 sodium, a G-modified inhibitory oligonucleotide (INH-ODN), is a selective TLR7 inhibitor. ODN 105871 can be uesd for inflammatory immune responses research.
    ODN 105871 sodium
  • HY-160228
    ORN 02
    		Activator
    ORN 02 is a synthetic single-stranded U-rich RNA and contains 6 repeats of UUAU sequence motif. The AU-rich oligoribonucleotides (ORNs) are able to stimulate TLR8.
    ORN 02
  • HY-P2036
    FSL-1
    		Agonist
    FSL-1, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection.
    FSL-1
  • HY-148511
    Vidutolimod
    		Agonist
    Vidutolimod (CMP-001) is a CpG-A oligodeoxynucleotide. Vidutolimod is a Toll-like receptor 9 (TLR9) agonist, which activates plasmacytoid dendritic cells (pDCs) and triggers interferon alpha (IFNα) release, leading to a cascade of anti-tumor immune effects.
    Vidutolimod
  • HY-168159
    TLR7 agonist 27
    		Agonist
    TLR7 agonist 27 (compound 24) is a potent TLR7 agonist with an EC50 of 238.1 nM. TLR7 agonist 27 shows weak agonistic activity against NOD2 (nucleotide-binding oligomerization domain 2) (EC50 of 6.2 μM). TLR7 agonist 27 is a potent immunostimulant, and can be used as a vaccine adjuvant and/or immunotherapeutic.
    TLR7 agonist 27
  • HY-D1056C3
    Lipopolysaccharides, from S. enterica serotype typhimurium
    		Activator
    Lipopolysaccharides, from S. enterica serotype typhimurium, are a kind of lipid-polysaccharide endotoxin. Smooth Gram-negative bacteria's lipopolysaccharides are made up of three components: lipid A, core oligosaccharide, and O antigen (OAg). The O antigen is a polymer of sugar repeat units (RUs); the Wzz protein regulates the length of the O antigen in lipopolysaccharides, and the number of RUs attached to lipid A is determined by the modal value set by the Wzz protein. S. enterica typhimurium has two Wzz proteins: WzzST (which makes the modal range of the O antigen between 16 and 35 RUs) and WzzfepE (which makes the modal value over 100 RUs). Mutating the genes corresponding to these two proteins causes the formation of short-chain O antigen chains and significantly reduces bacterial pathogenicity.
    Lipopolysaccharides, from S. enterica serotype typhimurium
  • HY-N0392R
    Polygalasaponin F (Standard)
    		Inhibitor
    Polygalasaponin F (Standard) is the analytical standard of Polygalasaponin F. This product is intended for research and analytical applications. Polygalasaponin F, an oleanane-type triterpenoid saponin extracted from Polygala japonica, decreases the release of the inflammatory cytokine tumor necrosis factor a (TNFa). Polygalasaponin F reduces neuroinflammatory cytokine secretion through the regulation of the TLR4-PI3K/AKT-NF-kB signaling pathway .
    Polygalasaponin F (Standard)
  • HY-107352R
    Fosfenopril (Standard)
    		Inhibitor
    Fosfenopril (Standard) is the analytical standard of Fosfenopril. This product is intended for research and analytical applications. Fosfenopril (Fosinoprilat) is a potent angiotensin converting enzyme (ACE) inhibitor. Fosfenopril alleviates lipopolysaccharide (LPS)-induced inflammation by inhibiting TLR4/NF-κB signaling in monocytes.
    Fosfenopril (Standard)
  • HY-D1056C4
    Lipopolysaccharides, from S. enterica serotype abortus equi
    		Activator
    Lipopolysaccharides are lipopolysaccharide endotoxins and TLR-4 activators that activate pathogenicity-associated molecular patterns (PAMPs) of the immune system and induce cell secretion of migrasomes. Lipopolysaccharides can be extracted from the outer leaflet of the outer membrane of Gram-negative bacteria and are composed of an antigenic O-specific chain, a core oligosaccharide, and lipid A. Lipopolysaccharides (LPS), from S. enterica serotype abortus equi is a kind of endotoxins derived from S. enterica serotype abortus equi.
    Lipopolysaccharides, from S. enterica serotype abortus equi
  • HY-153900
    TLR8 agonist 6
    		Agonist
    TLR8 agonist 6 (Compound A) is a TLR8 agonist, with an EC50 of 0.052 μM. TLR8 agonist 6 induces IL-12p40 production in human PBMC (EC50: 0.031 μM). TLR8 agonist 6 can be used in the research of virus resistance, infection resistance, autoimmunity, tumor, etc.
    TLR8 agonist 6
  • HY-N0703R
    Schaftoside (Standard)
    		Inhibitor
    Schaftoside (Standard) is the analytical standard of Schaftoside. This product is intended for research and analytical applications. Schaftoside is a flavonoid found in a variety of Chinese herbal medicines, such as Eleusine indica. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission.
    Schaftoside (Standard)
  • HY-N12110
    SMU-CX1
    		Inhibitor
    SMU-CX1 is a specific TLR3 inhibitor (IC50: 0.11 μM) with IC50 ranging from 0.14-0.33 μM against multiple influenza A virus subtypes. SMU-CX1 inhibits the viral PB2 and NP proteins with an IC50 of 0.43 μM for SARS-CoV-2 activity. SMU-CX1 also inhibits inflammatory factors in host cells, including IFN-β, IP-10, and CCL-5.
    SMU-CX1
  • HY-150738A
    Biotin-labeled ODN 2088 sodium
    Biotin-labeled ODN 2088 (sodium) is a potent TLR3, TLR7 and TLR9 inhibitor. Biotin-labeled ODN 2088 (sodium) can be used to evaluate CpG ODN cellular uptake and localization using a biotin detection system and light microscopy.
    Biotin-labeled ODN 2088 sodium
  • HY-135811
    Desethyl chloroquine
    		Inhibitor
    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
  • HY-P10586
    Macrophage-activating lipopeptide 2
    		Activator
    Macrophage-activating lipopeptide 2 (MALP-2) is an agonist of Toll like receptors TLR-2/TLR-6. Macrophage-activating lipopeptide-2 can enhance endothelial nitric oxide synthase (eNOS) phosphorylation and endothelial cell release of NO, thereby improving vasodilation. Macrophage-activating lipopeptide-2 can enhance endothelial adhesion of white blood cells and improve perfusion recovery and collateral growth in the hind limbs of hypercholesterolemic Apoe deficient mice undergoing experimental femoral artery ligation (FAL).
    Macrophage-activating lipopeptide 2
  • HY-17589S
    Chloroquine-d5 diphosphate
    		Inhibitor
    Chloroquine-d5 (diphosphate) is the deuterium labeled Chloroquine (phosphate). Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
    Chloroquine-d<sub>5</sub> diphosphate
  • HY-159670A
    Monophosphoryl Lipid A-12 free acid
    		Agonist
    Monophosphoryl Lipid A-12 (free acid) is a toll-like receptor 4 agonist. Monophosphoryl Lipid A-12 (free acid) can be used for the research of immunization and vaccine.
    Monophosphoryl Lipid A-12 free acid
  • HY-D1056A4
    Lipopolysaccharides, from E. coli O128:B12
    		Activator
    Lipopolysaccharides, from E. coli O128:B12 is commonly used to stimulate the inflammatory pathway in an infection/inflammation induced preterm animal model. Specific Lipopolysaccharides from E. coli serotypes induce activation of different inflammatory pathways in the neonatal rat brain. Compared with other Escherichia coli, Lipopolysaccharides (O111:B4, O55:B5, O127:B8), Lipopolysaccharides, from E. coli O128:B12 has lower induction efficiency of inflammation. Cub survival rate was 100% after the treatment.
    Lipopolysaccharides, from E. coli O128:B12
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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