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-146244
    Agatolimod
    Agonist
    Agatolimod (ODN 2006), a class B ODN (oligodeoxynucleotide), is a TLR9 agonist. Agatolimod is also an optimal CpG sequence for humans. Agatolimod stimulates very strong production of NO2 and IL-6 in HD11 cells. Agatolimod can be used for breast cancer research. Sequence: 5'-tcgtcgttttgtcgttttgtcgtt-3'.
    Agatolimod
  • HY-109104
    Telratolimod
    Agonist 98.98%
    Telratolimod (MEDI9197) is a potent toll like receptors 7/8 (TLR7/8) agonist, with antitumor activity.
    Telratolimod
  • HY-123942
    Diprovocim
    Agonist 98.35%
    Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC50=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses.
    Diprovocim
  • HY-107575
    TLR4-IN-C34
    Inhibitor 99.85%
    TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.
    TLR4-IN-C34
  • HY-15601
    Vesatolimod
    Agonist 99.90%
    Vesatolimod (GS-9620) is a potent, selective and orally active agonist of Toll-Like Receptor (TLR7) with an EC50 of 291 nM.
    Vesatolimod
  • HY-108471
    CU-CPT22
    Inhibitor ≥99.0%
    CU-CPT22 is a potent protein complex of toll-like receptor 1 and 2 (TLR1/2) inhibitor, and competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with a Ki of 0.41 µM. CU-CPT22 blocks Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 µM.
    CU-CPT22
  • HY-13773
    Motolimod
    Agonist 98.12%
    Motolimod (VTX-2337;VTX-378) is a selective Toll-like receptor 8 (TLR8) agonist, with an EC50 of approximately 100 nM.
    Motolimod
  • HY-P9930
    Evolocumab
    Inhibitor 98.40%
    Evolocumab (AMG 145) is a human monoclonal antibody that inhibits PCSK9. Evolocumab is used in the study of hypercholesterolemia and atherosclerotic cardiovascular disease. Evolocumab binds to circulating PCSK9 protein and inhibits its binding to LDLR. Evolocumab has antioxidant and cytoprotective activities against H2O2-induced oxidative damage to endothelial cells. Evolocumab may also negatively regulate activation of the TLR-4/NF-κB signaling pathway to prevent inflammation.
    Evolocumab
  • HY-150741
    ODN 2216
    Agonist
    ODN 2216 is a human-specific TLR9 (toll-like receptor 9) ligand or agonist. ODN 2216 induces high amounts of IFN-α and IFN-β. ODN 2216 induces IFN-α by pDC (plasmacytoid DC) and IL-12 (p40) production by DC (dendritic cells). ODN 2216 stimulates IFN-γ production in peripheral blood mononuclear cells (PBMC), which is indirect and mediated by IFN-α/β. ODN 2216 can activate NK cells and promote IFN-γ production of TCR-triggered CD4+ T cells.
    ODN 2216
  • HY-150724
    ODN 1018
    Agonist
    ODN 1018 (1018 ISS), an oligodeoxynucleotide, is a TLR-9 agonist. ODN 1018 is also a synthetic immunostimulatory sequence that can be used as vaccine adjuvant. Sequence: 5′-TGACTGTGAACGTTCGAGATGA-3′.
    ODN 1018
  • HY-116961
    TH1020
    Antagonist 99.60%
    TH1020 is a potent and selective toll-like receptor 5 (TLR5)/flagellin complex antagonist with an IC50 of 0.85 μM. TH1020 inhbits flagellin-induced TLR5 signaling. TH1020 is inactive against TLR2, TLR3, TLR4, TLR7 and TLR8.
    TH1020
  • HY-141537
    ABR-238901
    Inhibitor 99.25%
    ABR-238901 is an orally active and potent S100A8/A9 blocker and inhibits S100A8/A9 interaction with its receptors RAGE (receptor for advanced glycation endproducts) and TLR4 (toll-like receptor 4). ABR-238901 has the potential for myocardial infarction (MI) research.
    ABR-238901
  • HY-P2565
    Pepinh-TRIF TFA
    Inhibitor 98.68%
    Pepinh-TRIF (TFA) is a 30 aa peptide that blocks TIR-domain-containing adapter-inducing interferon-β (TRIF) signaling by interfering with TLR-TRIF interaction.
    Pepinh-TRIF TFA
  • HY-135748
    Polyinosinic-polycytidylic acid sodium
    Agonist ≥99.0%
    Polyinosinic-polycytidylic acid (Poly(I:C)) sodium 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 sodium can directly trigger cancer cells to undergo apoptosis.
    Polyinosinic-polycytidylic acid sodium
  • HY-124603
    AT791
    Inhibitor 98.77%
    AT791 is a potent and orally bioavailable TLR7 and TLR9 inhibitor. AT791 inhibits TLR7 and 9 signaling in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro.
    AT791
  • HY-109137
    Selgantolimod
    Agonist 98.23%
    Selgantolimod (GS-9688) is an orally active, potent and selective toll-like receptor 8 (TLR8) agonist for the treatment of hepatitis B virus (HBV) and human immunodeficiency virus (HIV) infection.
    Selgantolimod
  • HY-139567
    Afimetoran
    Antagonist 98.17%
    Afimetoran is a toll-like receptor antagonist, which can be used in the research of inflammatory and autoimmune diseases.
    Afimetoran
  • HY-N0201
    Atractylenolide I
    Antagonist 99.87%
    Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
    Atractylenolide I
  • HY-112146
    MMG-11
    Antagonist 99.11%
    MMG-11 is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 inhibits both TLR2/1 and TLR2/6 signaling with IC50s of 1.7 µM for Pam3CSK4-induced hTLR2/1 and 5.7 µM for Pam2CSK4-induced hTLR2/6 responses.
    MMG-11
  • HY-110353
    CU-T12-9
    Agonist 98.94%
    CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
    CU-T12-9
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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