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-178169
    ETI60
    		Inhibitor
    ETI60 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.68 μM) and TLR9 (IC50 = 0.12 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI60 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI60 modulates the expression of genes associated with inflammation. ETI60 effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI60 can be used for autoimmune and inflammatory diseases research.
    ETI60
  • 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-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 99.22%
    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-N15893
    α-Galactosyl FP20 sodium
    α-Galactosyl FP20 sodium, a TLR-4 agonist, is a vaccine adjuvant.
    α-Galactosyl FP20 sodium
  • HY-RS14591
    Tlr6 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Tlr6 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Tlr6 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Tlr6 Mouse Pre-designed siRNA Set A
  • HY-N16024
    FP-20 sodium
    		Agonist
    FP-20 sodium, a selective TLR4 agonist, is a vaccine adjuvant. FP-20 sodium induces MAPK- and NLRP3-dependent inflammasome activation. FP20 shows no toxicity in mouse vaccination experiments with OVA antigen and induces IgG production.
    FP-20 sodium
  • HY-RS14577
    Tlr1 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Tlr1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Tlr1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Tlr1 Mouse Pre-designed siRNA Set A
  • HY-P10982
    SjDX5-53
    		Inducer
    SjDX5-53 is a selective TLR2 inducer derived from a 3 kDa peptide from Schistosoma japonicum eggs. SjDX5-53 inhibits inflammatory Th1 and Th17 responses by inducing tolerogenic dendritic cells (tolDCs) and promoting the generation of regulatory T cells (Tregs) and their suppressive capacity. SjDX5-53 is primarily used in the treatment of autoimmune and inflammatory diseases such as colitis and psoriasis.
    SjDX5-53
  • 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, from S. enterica (Salmonella enterica) serotype Abortusequi are lipopolysaccharide endotoxins and TLR-4 activators derived from the Abortusequi serotype of S. enterica, classified as a mutated R-type LPS, which can activate pathogen-associated molecular patterns (PAMP) of the immune system and induce cellular secretion of migrasomes. Lipopolysaccharides, from S. enterica serotype abortus equi consist of core oligosaccharide (core oligosaccharide) and lipid A (Lipid A). S. enterica serotype Abortusequi is a major pathogen causing abortion in mares and is also associated with neonatal sepsis, multiple abscesses, orchitis, and polyarthritis in equids. It is primarily grouped based on lipopolysaccharides (O-antigen) and flagellin (H-antigen).
    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 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-101132A
    (Rac)-VB-201
    		Inhibitor
    (Rac)-VB-201 is the racemate of VB-201, an oxidized phospholipid small molecule that inhibits CD14- and toll-like receptor 2-dependent innate cell activation and suppresses atherosclerosis.
    (Rac)-VB-201
  • 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-P2358A
    PSMα3 TFA
    		Inhibitor
    PSMα3 TFA is a peptide for manipulating DCs to become tolerogenic for DC vaccination strategies. PSMα3 TFA penetrates and modulates human monocyte-derived DCs by altering the TLR2- or TLR4-induced maturation, inhibiting pro- and anti-inflammatory cytokine production and reducing antigen uptake. PSMα3 TFA is an important toxin released by the most virulent strains of methicillin-resistant Staphylococcus aureus (MRSA).
    PSMα3 TFA
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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