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-B0012
    Pamidronic acid
    		Inhibitor 99.05%
    Pamidronic acid, the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronic acid significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of OPG in cartilage and subchondral bone, and inhibiting the expression of RANKL and MMP-9 in both tissues, as well as TLR-4 in cartilage, thereby alleviating cartilage degeneration. Additionally, Pamidronic acid can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma.
    Pamidronic acid
  • HY-138139B
    AXC-715 trihydrochloride
    		Agonist 99.76%
    AXC-715 (T785) trihydrochloride is a TLR7/TLR8 dual agonist, extracted from patent WO2020168017 A1. AXC-715 trihydrochloride, compound D from WO2020190734A1, can be used for synthesis of antibody-adjuvant immunoconjugates, comprising an antibody construct that binds programmed death-ligand 1 (PD-L1) linked to one or more adjuvants.
    AXC-715 trihydrochloride
  • HY-20457
    TL8-506
    		Agonist
    TL8-506 is a specific TLR8 agonist with an EC50 of 30 nM. TL8-506 has immunomodulatory effects and can be used in the study of tuberculosis and cancer immunotherapy.
    TL8-506
  • HY-P99008
    Atibuclimab
    		Inhibitor
    Atibuclimab, is a chimeric monoclonal antibody directed against CD14 and is composed of murine variable and human IgG4 Fc regions. Atibuclimab can be used for the research of amyotrophic lateral sclerosis. Atibuclimab attenuates LPS-induced symptoms and strongly inhibits LPS-induced proinflammatory cytokine release, while only delaying the release of the anti-inflammatory cytokines soluble TNF receptor type I and IL-1 receptor antagonist.
    Atibuclimab
  • 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 98.87%
    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-126154
    L48H37
    		Inhibitor
    L48H37 is an analog of Curcumin (HY-N0005) with improved chemical stability. L48H37 is a potent and specific myeloid differentiation protein 2 (MD2) inhibitor and inhibits the interaction and signaling transduction of LPS-TLR4/MD2. L48H37 is used for the research of sepsis or lung injury treatment.
    L48H37
  • HY-112050
    CU-CPT-8m
    		Antagonist 99.98%
    CU-CPT-8m is a specific TLR8 antagonist, with an IC50 of 67 nM.
    CU-CPT-8m
  • HY-150217
    CpG ODN 10101
    		Agonist
    CpG ODN 10101, a synthetic oligodeoxynucleotide (ODN),  is a toll-like receptor 9 (TLR9) agonist. CpG ODN 10101 is a potent inducer of cytokine/chemokine expression ex vivo when used in combination with HH2(VQLRIRVAVIRA-NH2). CpG ODN 10101 induces IFN- secretion from dendritic cells (DCs) and stimulates B-cells.CpG ODN 10101 has antiviral and immunomodulatory properties that can influence chronic infection with HCV.
    CpG ODN 10101
  • HY-112667
    CU-CPT-9a
    		Antagonist 99.36%
    CU-CPT-9a is a specific TLR8 antagonist, with an IC50 of 0.5 nM.
    CU-CPT-9a
  • 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-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-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-135905
    CL264
    		Inhibitor 98.63%
    CL264 is a TLR7-specific agonist for innate immune signals research.
    CL264
  • 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-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-18976
    UF010
    		99.84%
    UF010 is a selective inhibitor of class I HDAC. UF010 has cytotoxicity to cancer cells and reduces neuroinflammation in the hippocampus. UF010 can be used for the research of neurological diseases.
    UF010
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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