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-163670
    TLR7 agonist 21
    		Inhibitor
    TLR7 agonist 21 (Compound 27B) is a selective agonist for Toll-like receptor 7(TLR7), with an EC50 of 17.53 nM (for human TLR7) and 41.7 nM (for mouse TLR7). TLR7 agonist 21 stimulates the secretion of pro-inflammatory cytokines, such as IL-6, TNF-α, IFN-α1, and IL-4. TLR7 agonist 21 acts as a vaccine adjuvant, increases levels of IgG and IgA, and protects the mouse from influenza virus infections.
    TLR7 agonist 21
  • HY-162725
    TLR7 agonist 24
    		Agonist
    TLR7 agonist 24 (Compound 21) is an agonist for TLR7 with EC50 of 3.72 μM. TLR7 agonist 24 can be used as a vaccine adjuvant when combined with Aluminum Hydroxide (HY-B1521), that enhances the immune response against SARS-CoV-2 and hepatitis B antigens.
    TLR7 agonist 24
  • HY-N16020
    α-Glucosyl FP20 sodium
    α-Glucosyl FP20 sodium, a TLR-4 agonist, is a vaccine adjuvant.
    α-Glucosyl FP20 sodium
  • HY-170770
    TLR7/8 agonist 12
    		Agonist
    TLR7/8 agonist 12 (compound 9) is an hTLR7/8 agonist, with EC50 values of 11 nM (hTLR7) and 150 nM (hTLR8), respectively. TLR7/8 agonist 12 has the potential for immunomodulation.
    TLR7/8 agonist 12
  • HY-D1056A5
    Lipopolysaccharides, from E. coli K-235
    		Activator
    Lipopolysaccharides, from E. coli (Escherichia coli) K-235 are lipopolysaccharide endotoxins and TLR-4 activators derived from E. coli, 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 E. coli K-235 exhibit a typical three-part structure: O-antigen (O-antigen), core oligosaccharide (core oligosaccharide), and lipid A (Lipid A). Lipopolysaccharides, from E. coli K-235 have a mitogenic effect on C57BL/10ScN spleen cells. Additionally, LPS purified using butanol and deoxycholic acid methods stimulates spleen cells in C57BL/10ScCR and C3H/HeJ mice.
    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 E. coli K-235
  • HY-152726
    TLR7 agonist 9
    		Agonist
    TLR7 agonist 9 (compound 10) is an aonist of TLR7. TLR7 agonist 9 can be used for research of cancer and infectious disease. TLR7 agonist 9 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    TLR7 agonist 9
  • HY-161629
    TLR8 agonist 7
    		Agonist
    TLR8 agonist 7 (Compound II-36) is an agonist for Toll-like receptor 8 (TLR8) with EC50 <250 nM. TLR8 agonist 7 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 7 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 98%.
    TLR8 agonist 7
  • HY-RS14582
    Tlr2 Rat Pre-designed siRNA Set A
    		Inhibitor

    Tlr2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Tlr2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Tlr2 Rat Pre-designed siRNA Set A
  • 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-P11250
    HVF18-a3-d
    		Inhibitor
    HVF18-a3-d is an antimicrobial peptide. HVF18-a3-d reduces NO production. HVF18-a3-d inhibits the production of TNF-α and IL-6, reduces ROS production, and suppresses the TLR4 signaling pathway, as well as LPS-induced phosphorylation of ERK, JNK, and p38 MAPK. HVF18-a3-d exhibits antimicrobial activity against a variety of bacteria by disrupting their outer and inner membranes. HVF18-a3-d protects mice from fatal septic shock induced by Acinetobacter baumannii resistant to Carbapenem. HVF18-a3-d shows anti-inflammatory and antioxidant effects.
    HVF18-a3-d
  • 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-165386
    TU-100
    		Inhibitor
    TU-100 is a Japanese herbal medicine. TU-100 exhibits anti-cancer effects by regulating cancer-associated fibroblasts (CAFs) in the TME. TU-100 can antagonize the M2 polarization phenotype of macrophages in the tumor microenvironment by suppressing the TLR4/NF-κB/STAT3 axis. TU-100 can inhibit the high expression of MMP-2, COX-2, and VEGF in TAMs.
    TU-100
  • HY-129684
    IAXO-101 iodide
    		Inhibitor
    IAXO-101 (iodide) is a TLR4/CD14 blocker. IAXO-101 (iodide) can inhibit the innate immune pathway of CD14. IAXO-101 (iodide) is capable of improving the recording performance of intracortical microelectrodes in mice. IAXO-101 (iodide) can also partially alleviate fetal growth restriction, placental vascular damage, and reduce the level of the inflammatory factor TNF-α in pregnant mice infected with malaria. IAXO-101 (iodide) can be used in the research of gestational malaria and inflammatory diseases.
    IAXO-101 iodide
  • 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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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