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-153072
    TLR7 agonist 7
    		Agonist
    TLR7 agonist 7 (compound IIb-26) is an TLR7 agonist with an EC50 value of ~4 nM.
    TLR7 agonist 7
  • HY-134958
    Polyinosinic-polycytidylic acid potassium
    		Agonist
    Polyinosinic-polycytidylic acid potassium (Poly(I:C) potassium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid potassium can directly trigger cancer cells to undergoApoptosis.
    Polyinosinic-polycytidylic acid potassium
  • HY-175782
    SMU-R39
    		Antagonist
    SMU-R39 is a TLR7 and TLR8 antagonist with IC50 values of 3.22 μM and 0.24 μM, respectively. SMU-R39 binds to recombinant mTLR7 protein (KD = 2.36 μM) and to recombinant hTLR8 protein (KD = 105 nM). SMU-R39 suppresses downstream NF-κB and MAPK signaling, and reduces secretion/transcription of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in PBMCs and THP-1 cells. SMU-R39 demonstrates anti-inflammatory efficacy in Imiquimod (IMQ) (HY-B0180)-induced psoriasis mouse model. SMU-R39 can be used for the study of autoimmune diseases such as psoriasis.
    SMU-R39
  • 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-N15936
    a15:0-i15:0 PE
    		Agonist
    a15:0-i15:0 PE is a diacyl phosphatidylethanolamine with two branched chains. a15:0-i15:0 PE is a non-canonical TLR2-TLR1 heterodimer agonist and has immunogenic activity. a15:0-i15:0 PE activates T cells and DC signaling and shows anti-inflammatory activity. a15:0-i15:0 PE induces TNFα and IL-6 production. a15:0-i15:0 PE is a the major component (approximately 50%) of A. muciniphila’s lipid membrane.
    a15:0-i15:0 PE
  • 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 stock solution of ≥2 mg/mL and ensure that it is fully mixed and dissolved. Due to the adsorption characteristics of LPS, low adsorption centrifuge tubes should be used for aliquoting and storage.
    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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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