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-12756A
    E6446 dihydrochloride
    		Antagonist 99.96%
    E6446 dihydrochloride is a potent and orally acitve TLR7 and TLR9 antagonist, used in the research of deleterious inflammatory responses. E6446 dihydrochloride is also a potent SCD1 inhibitor (KD: 4.61 μM), significantly inhibiting adipogenic differentiation and hepatic lipogenesis through SCD1-ATF3 signaling. E6446 dihydrochloride also improves liver pathology in high-fat diet (HFD)-fed mice and may be useful in the study of non-alcoholic fatty liver disease (NAFLD).
    E6446 dihydrochloride
  • HY-N0741A
    Leonurine hydrochloride
    		99.43%
    Leonurine hydrochloride is an alkaloid isolated from Leonurus artemisia, with anti-oxidative and anti-inflammatory.
    Leonurine hydrochloride
  • HY-135748A
    Poly (I:C):Kanamycin (1:1) (sodium)
    		Agonist
    Poly (I:C):Kanamycin (1:1) sodium is an isometric complex of Poly (I:C) (HY-135748) and Kanamycin (HY-16566). Poly(I:C) sodium, a synthetic analog of double-stranded RNA, is a TLR3 and retinoic acid-inducible gene I receptor (RIG-I and b>MDA5) agonist. Poly(I:C) sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses and induce apoptosis in cancer cells. Kanamycin is an orally active antibacterial agent (Gram-negative/positive bacteria) that inhibits translocation and causes miscoding by binding to the 70S ribosomal subunit. Kanamycin shows good inhibitory activity against Mycobacterium tuberculosis (susceptible and drug-resistant) and Klebsiella pneumoniae, and can be used in the research of tuberculosis and pneumonia.
    Poly (I:C):Kanamycin (1:1) (sodium)
  • HY-103698A
    TLR7/8 agonist 1 dihydrochloride
    		Agonist 99.70%
    TLR7/8 agonist 1 dihydrochloride is a toll-like receptor TLR7/TLR8 dual-agonistic imidazoquinoline.
    TLR7/8 agonist 1 dihydrochloride
  • HY-N1346
    Robinin
    		Inhibitor 98.77%
    Robinin is a flavonoid that can be extracted from the leaves of purple cowpea, inhibiting TGF-β, TLR4/NF-κB and TLR2-PI3k-AKT signaling pathways. Robinin exerts anti-inflammatory and anti-tumor effects. The combination of Robinin and Methotrexate (HY-14519) reduces inflammation in experimental arthritis, Robinin can decrease the Doxorubicin (HY-15142A) induced cardiac toxicity effect.
    Robinin
  • HY-N0726
    Dracorhodin perchlorate
    		Modulator 99.14%
    Dracorhodin perchlorate (Dracohodin perochlorate) is a natural product. Dracorhodin perchlorate can be obtained from the natural active molecule Dragon's blood. Dracorhodin perchlorate inhibits PI3K/Akt and NF-κB activation, upregulates p53 expression, activates caspase, produces ROS, and promotes Apoptosis. Dracorhodin perchlorate regulates the TLR4. Dracorhodin perchlorate promotes wound healing, improves diabetes. Dracorhodin perchlorate has anti-tumor activity against prostate cancer, breast cancer, cervical cancer and other cancers.
    Dracorhodin perchlorate
  • HY-103697A
    Gardiquimod diTFA
    		≥99.0%
    Gardiquimod diTFA is an imidazoline TLR7/8 agonist. Gardiquimod diTFA inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 at concentrations below 10 μM.
    Gardiquimod diTFA
  • 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-124750
    NecroX-7
    		Inhibitor 99.69%
    NecroX-7 is a potent free radical scavenger and a HMGB1 (high-mobility group box 1) inhibitor. NecroX-7 can be used as an antidote to acetaminophen toxicity. NecroX-7 exerts a protective effect by preventing the release of HMGB1 in ischemia/reperfusion injury. NecroX-7 inhibits the HMGB1-induced release of TNF and IL-6, as well as the expression of TLR-4 and receptor for advanced glycation end products. NecroX-7 can be used graft-versus-host disease (GVHD) research.
    NecroX-7
  • HY-108472
    Loxoribine
    		Agonist 99.64%
    Loxoribine (7-Allyl-8-oxoguanosine) is a guanosine analog with anti-viral and anti-tumor activities. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist.
    Loxoribine
  • HY-150751C
    ODN TTAGGG sodium
    		Antagonist
    ODN TTAGGG sodium, inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG sodium is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG sodium can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3'.
    ODN TTAGGG sodium
  • 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-130320
    Monophosphoryl lipid A
    		Agonist ≥99.0%
    Monophosphoryl lipid A (Glucopyranosyl lipid A) is a toll-like receptor 4 agonist. Monophosphoryl lipid A is derived from the cell wall of nonpathogenic Salmonella. Monophosphoryl lipid A can be used for the research of immunization and vaccine.
    Monophosphoryl lipid A
  • 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-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-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-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-18325
    AN-3485
    		Inhibitor
    AN-3485 is a benzoxaborole analogue and an orally active antagonist of the Toll-like pathway. AN-3485 can inhibit TLR-mediated inflammatory cytokine secretion and has significant anti-inflammatory activity. In addition, AN-3485 also has certain anti-tumor activity.
    AN-3485
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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