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-D1056B3
    Lipopolysaccharides, from Klebsiella pneumoniae
    Activator
    Lipopolysaccharides, from Klebsiella, are lipopolysaccharide endotoxins. Lipopolysaccharides, from Klebsiella pneumoniae, consist of three parts: lipid A, core oligosaccharide, and O-specific antigen or O-side chain. In smooth LPS, the core region is divided into two areas: the inner core near the lipid A and the outer core that provides attachment sites for the O-antigen. In the lipopolysaccharide of Klebsiella pneumoniae, the l,d-HeppII at the O-3 position can be replaced by an α-d-galacturonic acid residue (α-d-GalpA). In most studied Enterobacteriaceae, the core LPS contains inner core phosphorylation modifications, but the core LPS of Klebsiella pneumoniae lacks this modification. The unique core structure plays an important role in the outer membrane permeability and pathogenesis of Klebsiella pneumoniae.
    Lipopolysaccharides, from Klebsiella pneumoniae
  • HY-135042
    CAY10614
    Antagonist 98.04%
    CAY10614 is a potent TLR4 antagonist. CAY10614 inhibits the lipid A-induced activation of TLR4, with an IC50 of 1.675 μM. CAY10614 can improve survival of mice in lethal endotoxin shock model.
    CAY10614
  • HY-130797
    TLR7/8 agonist 3
    Agonist 99.96%
    TLR7/8 agonist 3 is a potent TLR7 and TLR8 agonist, extracted from patent WO2016057618 (compound of formula (II)).
    TLR7/8 agonist 3
  • HY-110120
    DSR-6434
    Agonist 99.55%
    DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect.
    DSR-6434
  • HY-20457
    TL8-506
    Agonist
    TL8-506 is a specific TLR8 agonist with an EC50 of 30 nM. TL8-506 can be used for the research of tuberculosis and autoimmune diseases.
    TL8-506
  • HY-128598
    MD2-TLR4-IN-1
    Inhibitor 99.62%
    MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively.
    MD2-TLR4-IN-1
  • HY-N2345
    Procyanidin B3
    Inhibitor 99.92%
    Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis.
    Procyanidin B3
  • HY-101929
    CU-CPT17e
    Agonist 99.00%
    CU-CPT17e is a potent multi-Toll-like receptor (TLR) agonist that activates TLR3, TLR8, and TLR9.
    CU-CPT17e
  • HY-148980A
    Polyinosinic acid sodium
    Polyinosinic acid sodium is the sodium form of Polyinosinic acid (HY-148980). Polyinosinic acid is a single stranded homonucleic acid, which is a Toll-like Receptor 3 (TLR3) ligand. Polyinosinic acid enhances cellular immune response through TLR3 and TRIF. Polyinosinic acid has potential applications in immune regulation.
    Polyinosinic acid sodium
  • HY-N2055
    Kaempferol 3-O-sophoroside
    Inhibitor 99.84%
    Kaempferol 3-O-sophoroside is an orally active derivative of Kaempferol. It exhibits anti-inflammatory, analgesic, and antidepressant effects. Kaempferol 3-O-sophoroside is an inhibitor of the cell surface receptor toll-like receptor (TLR) 2/4 for High mobility group box 1 (HMGB1), and it also exerts anti-inflammatory effects by blocking the activation of NF-κB expression and the production of TNF-α. Kaempferol 3-O-sophoroside promotes the production of brain-derived neurotrophic factor (BDNF) and enhances autophagy by binding to AMP-activated protein kinase (AMPK), thereby exerting antidepressant effects. Kaempferol 3-O-sophoroside holds promise for research in the fields of inflammation and neurodegenerative diseases.
    Kaempferol 3-O-sophoroside
  • HY-131952
    TLR7/8/9-IN-1
    Antagonist 98.51%
    TLR7/8/9-IN-1 is a potent and orally bioavailable small molecule antagonist (IC50 = 43 nM) of Toll-like receptors 7/8/9 (TLR7/8/9).
    TLR7/8/9-IN-1
  • HY-117602
    TLR7 agonist 3
    Agonist 99.90%
    TLR7 agonist 3 (Compound 2) is a potent agonist of toll-like receptor 7 (TLR7). TLR7 has an important role in immune activation processes and represents an emerging agent discovery target for the development of immunomodulators.
    TLR7 agonist 3
  • HY-18325
    AN-3485
    Inhibitor
    AN-3485 is a benzoxaborole analog, Toll-Like Receptor(TLR) inhibitor with IC50 values ranging from 18 to 580 nM.
    AN-3485
  • HY-160229
    ssRNA40 sodium
    Activator
    ssRNA40 (sodium) is a 20-mer phosphothioate protected single-stranded RNA oligonucleotide. ssRNA40 is a uridine-rich ssRNA derived from the HIV-1 long terminal repeat on activation of NK cells via TLR7/8[1][2].
    ssRNA40 sodium
  • HY-W082785A
    L6H21
    Inhibitor 99.46%
    L6H21, a Chalcone (HY-121054) derivative, is an orally active, potent and specific myeloid differentiation 2 (MD-2) inhibitor. L6H21 directly binds to MD-2 protein with a high affinity and low KD value of 33.3?μM, blocking the formation of the LPS-TLR4/MD-2 complex. L6H21 inhibits LPS-induced expression of TNF-α and IL-6 in RAW264.7 macrophages, with IC50 values of 6.58 and 8.59 μM, respectively. L6H21 can be used for alcoholic liver disease, metabolic disturbance and neuroinflammation research.
    L6H21
  • 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-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-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-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-150748A
    ODN D-SL01 sodium
    99.94%
    ODN D-SL01 sodium, a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. ODN D-SL01 sodium has strong immunostimulatory activity in a variety of vertebrate species and has anticancer activity. ODN D-SL01 sequence: 5'- T-C-G-C-G-A-C-G-T-T-C-G-C-C-C-G-A-C-G-T-T-C-G-G-T-A-3'.
    ODN D-SL01 sodium
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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