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-W092043
    TLR4-IN-C34-C2-COOH
    		Inhibitor
    TLR4-IN-C34-C2-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34 (HY-107575). TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.
    TLR4-IN-C34-C2-COOH
  • HY-P2358
    PSMα3
    		98.45%
    PSMα3 is a peptide for manipulating DCs to become tolerogenic for DC vaccination strategies. PSMα3 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 is an important toxin released by the most virulent strains of methicillin-resistant Staphylococcus aureus (MRSA).
    PSMα3
  • HY-150750
    ODN M362
    		Agonist
    ODN M362, a class C oligodeoxynucleotide, is a TLR-9 agonist and can be used as a vaccine adjuvant. ODN M362 induces cancer cell apoptosis.
    ODN M362
  • HY-B0180B
    Imiquimod maleate
    		Agonist 99.25%
    Imiquimod maleate (R 837 maleate), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod maleate exhibits antiviral and antitumor effects in vivo. Imiquimod maleate can be used for the research of external genital, perianal warts, cancer and COVID-19.
    Imiquimod maleate
  • HY-109010
    Poseltinib
    		Inhibitor 98.08%
    Poseltinib (HM71224) is an orally active, selective, irreversible small molecule Bruton tyrosine kinase (BTK) inhibitor. With an IC50 of 1.95 nM. Poseltinib effectively inhibits the signaling mediated by B cell receptors (BCR), Fc receptors (FcR), and Toll-like receptors (TLR). Poseltinib has anti-inflammatory activity and can be used in the research of rheumatoid arthritis.
    Poseltinib
  • HY-153808B
    Complete Freund's adjuvant (CFA, 1 mg/ml)
    Complete Freund's adjuvant (CFA, 1 mg/ml) is an immunoadjuvant emulsified with antigen that can enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA, 1 mg/ml) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA, 1 mg/ml) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA, 1 mg/ml) stimulates a strong and durable immune response and can be used to induce rheumatoid arthritis in rats, and more.
    Complete Freund's adjuvant (CFA, 1 mg/ml)
  • HY-P1181A
    Pam2CSK4 TFA
    		Agonist 99.28%
    Pam2CSK4 (TFA), a lipopeptide, is a TLR6-independent TLR2 ligand and agonist. Pam2CSK4 (TFA) promotes platelet aggregation, and increases platelet adhesion to collagen-coated surfaces in a TLR2/NF-κB/BTK-dependent manner. Pam2CSK4 (TFA) also activates iNOS expression and NO production in mouse macrophages.
    Pam2CSK4 TFA
  • HY-131945
    CU-115
    		Antagonist 99.55%
    CU-115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU-115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells.
    CU-115
  • HY-153840A
    ODN INH 18 sodium
    		Inhibitor 99.76%
    ODN INH-18 sodium is a linear 24-mer class B INH-ODN in which the 5' INH-ODN 4084-F sequence was followed by a random stretch of 12 nucleotides lacking the ability to form significant secondary structures. ODN INH-18 sodium showes inhibitory potency for TLR9 ligand-induced IFN-α production.
    ODN INH 18 sodium
  • HY-150736
    ODN 20844
    		Inhibitor
    ODN 20844, a guanine-modified inhibitory oligonucleotide (INH-ODN), is a TLR7 and TLR9 (Toll-like receptor) inhibitor, and its parent is INH-ODN 2088. ODN 20844 disrupts TLR7- and TLR9-mediated immune cell immune responses. ODN 20844 sequence: 5'-TCCTGGCGc7GGGAAGT-3'.
    ODN 20844
  • HY-P10208A
    RKH acetate
    		Antagonist 99.45%
    RKH acetate exerts protective effects against sepsis-induced death and organ damage. RKH acetate can directly bind to Toll-like receptor 4 (TLR4) and block TLR4 signal transduction in immune cells.
    RKH acetate
  • HY-W105835
    Magnesium citrate
    		Modulator ≥98.0%
    Magnesium citrate (Trimagnesium dicitrate) is an orally active magnesium-containing compound that can cross the blood-brain barrier (BBB). Magnesium citrate can be used as an intestinal cleanser and is studied for its application in laxatives. Magnesium citrate can also increase the pain threshold and is studied for pain-relief purposes.
    Magnesium citrate
  • HY-148511A
    Vidutolimod sodium
    		Inhibitor
    Vidutolimod sodium is a CpG-A oligodeoxynucleotide. Vidutolimod sodium 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 sodium
  • HY-118250
    GSK2245035
    		Agonist 99.85%
    GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for asthma.
    GSK2245035
  • HY-D1056A2
    Lipopolysaccharides, from E. coli O127:B8
    		Activator
    Lipopolysaccharides, from E. coli O127:B8 (LPS, from Escherichia coli (O127:B8)) are endotoxins and TLR4 activators extracted from Escherichia coli (E. coli O127:B8) and are classified as S (smooth) type LPS. Lipopolysaccharides, from E. coli O127:B8 possess the typical three-part structure: O-antigen, R3-type core oligosaccharide, and lipid A. Lipopolysaccharides, from E. coli O127:B8 activate TLR-4 in immune cells, can induce inflammatory responses and ileal contractility, and can be used to construct intestinal inflammation models.
    Lipopolysaccharides, from E. coli O127:B8
  • HY-144501
    D18
    		Agonist 98.79%
    D18 is an immune modulator. D18 acts as a TLR7/8 dual agonist (EC50=24 nM for hTLR7 and 10 nM for hTLR8, respectively). D18 increases PD-L1 expression through epigenetic regulation, thus sensitizing tumors to PD-1/PD-L1 blockade. D18 is a ADC cytotoxin uesd for the systhesis of ADC HE-S2.
    D18
  • HY-107352
    Fosfenopril
    		Inhibitor 99.89%
    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
  • HY-146244A
    Biotin-labeled Agatolimod sodium
    Biotin-labeled Agatolimod (sodium), a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. Biotin-labeled Agatolimod (sodium) can be used to evaluate CpG ODN cellular uptake and localization using a biotin detection system and light microscopy.
    Biotin-labeled Agatolimod sodium
  • HY-112051
    CU-CPT9b
    		Antagonist 99.03%
    CU-CPT9b is a specific TLR8 antagonist, with an IC50 of 0.7 nM. CU-CPT9b shows high binding affinity towards TLR8 with a Kd of 21 nM.
    CU-CPT9b
  • HY-13740G
    Resiquimod (GMP)
    		Agonist
    Resiquimod (R848) (GMP) is Resiquimod (HY-13740) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist. Resiquimod (GMP) can induce human mMDSC to mature into inflammatory macrophages.
    Resiquimod (GMP)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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