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-D1056H
    Lipopolysaccharides, from S. marcescens
    		Activator
    Lipopolysaccharides, from S. marcescens (Serratia marcescens) are lipopolysaccharide endotoxins and TLR-4 activators derived from Serratia marcescens, classified as S-type LPS, which can activate pathogen-associated molecular patterns (PAMP) of the immune system and induce cellular secretion of migrasomes. Lipopolysaccharides, from S. marcescens exhibit a typical three-part structure: O-antigen (O-antigen), core oligosaccharide (core oligosaccharide), and lipid A (Lipid A). Lipopolysaccharides, from S. marcescens induce NF-κB activation in mouse cells via Toll-like receptor (TLR4)/MD-2. The lipopolysaccharides of S. marcescens can induce apoptosis in host immune cells, thereby suppressing the host's innate immunity.
    Lipopolysaccharides, from S. marcescens
  • HY-153254
    BMS905
    		Inhibitor 99.59%
    BMS905 is an orally active TLR7 and TLR8 dual inhibitor (IC50s: 0.7 and 3.2 nM respectively). BMS905 inhibits TLR7 or TLR8 induced IL-6 production in human/mouse whole blood. BMS905 can be used for research of lupus.
    BMS905
  • HY-B0012A
    Pamidronate disodium
    		Inhibitor ≥98.0%
    Pamidronate disodium (CGP 23339A), the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronate disodium significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of osteoprotegerin 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, Pamidronate disodium can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma.
    Pamidronate disodium
  • HY-B1370R
    Hydroxychloroquine (sulfate) (Standard)
    		Inhibitor 99.28%
    Hydroxychloroquine (sulfate) (Standard) is the analytical standard of Hydroxychloroquine (sulfate). This product is intended for research and analytical applications. Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro.
    Hydroxychloroquine (sulfate) (Standard)
  • HY-N0392
    Polygalasaponin F
    		Inhibitor 99.85%
    Polygalasaponin F, an oleanane-type triterpenoid saponin extracted from Polygala japonica, decreases the release of the inflammatory cytokine tumor necrosis factor a (TNFa). Polygalasaponin F reduces neuroinflammatory cytokine secretion through the regulation of the TLR4-PI3K/AKT-NF-kB signaling pathway .
    Polygalasaponin F
  • HY-W008634
    Bropirimine
    		Agonist 99.92%
    Bropirimine is a synthetic agonist for toll-like receptor 7 (TLR7). Bropirimine inhibits differentiation of osteoclast precursor cells into osteoclasts via TLR7-mediated production of IFN-β. Bropirimine is an orally active immunomodulator that has demonstrated anticancer activity in transitional cell carcinoma in situ (CIS) in both the bladder and upper urinary tract.
    Bropirimine
  • HY-100176
    PF-4878691
    		Agonist 99.89%
    PF-4878691 (3M-852A) is an orally active TLR7 agonist. PF-4878691 has the innate immune response activity, antiviral efficacy against HCV, and can be used for the research of cancer.
    PF-4878691
  • HY-139017
    TLR7/8 agonist 4
    		Agonist 99.04%
    TLR7/8 agonist 4 (compound 41) is a potent TLR7/8 agonist. TLR7/8 agonist 4 has anti-cancer activity.
    TLR7/8 agonist 4
  • HY-P99555
    Tomaralimab
    		Inhibitor
    Tomaralimab (OPN-305) is a humanised anti-TLR2 IgG4 monoclonal antibody. Tomaralimab has the potential for the research of Myelodysplastic Syndromes (MDS).
    Tomaralimab
  • HY-111269
    AZD8848
    		Agonist 99.14%
    AZD8848 is a selective toll-like receptor 7 (TLR7) anteagent agonist which is developed for the research of asthma and allergic rhinitis.
    AZD8848
  • HY-N6928
    Mogroside III-E
    		99.32%
    Mogroside III-E is a cucurbitane-type compound isolated from Siraitia grosvenorii, inhibits NO release, with anti-fibrotic activity.
    Mogroside III-E
  • HY-150746
    ODN 24991
    		Inhibitor
    ODN 24991, a guanine-modified inhibitory oligonucleotide (INH-ODN), is a TLR3, TLR7 and TLR9 (Toll-like receptor) inhibitor, and its parent is INH-ODN 2088. ODN 24991 disrupts TLR3-, TLR7- and TLR9-mediated immune cell immune responses. ODN 24991 sequence: 5'-C-C-T-G-G-C-c7rGm-G-G-G-3'.
    ODN 24991
  • HY-120149
    Inotodiol
    		Inhibitor
    Inotodiol activates p53 signaling pathway, inhibits MMP-2/9, and exhibits antitumor activity in cancer cell HeLa. Inotodiol inhibits the generation of ROS and exhibits antioxidant and neuroprotective effects. Inotodiol inhibits the activation of MAPK and NF-κB signaling pathway, and exhibits anti-inflammatory activity. Inotodiol inhibits TLR-4 mediated TNF-α production (IC50s in BMMC and BMDM is 0.7 μM and 3.0 μM), inhibits the degranulation in mast cell, exhibits anti-allergic activity. Inotodiol is orally active.
    Inotodiol
  • HY-150750A
    ODN M362 sodium
    ODN M362 sodium, a class C oligodeoxynucleotide, is a TLR-9 agonist and can be used as a vaccine adjuvant. ODN M362 sodium induces cancer cell apoptosis.
    ODN M362 sodium
  • HY-137345
    DB-3-291
    		Inhibitor 98.03%
    DB-3-291 is potent and selective PROTAC CSK degrader, with a Kd of 1 nM (Pink: CSK ligand (HY-131669); Blue: E3 ligase ligand (HY-103597); Black: linker (HY-N2407)).
    DB-3-291
  • HY-150742
    ODN 2336
    		Agonist
    ODN 2336 is a A-Class CpG ODN (oligodeoxynucleotides), is a potent TLR9 agonist. ODN 2336 induces the production of IFN-α. ODN 2336 up-regulates the expression of IP-10 mRNA and IL-18 mRNA. ODN 2336 can be used as adjuvant of vaccines.
    ODN 2336
  • HY-103639A
    M62812
    		Inhibitor 99.86%
    M62812 is a toll-like receptor 4 (TLR4) signaling inhibitor. M62812 inhibits endothelial and leukocyte activation and prevents lethal septic shock in mice. M62812 can reduces LPS-induced coagulation and inflammatory responses. M62812 can be used for the research of sepsis.
    M62812
  • HY-146195
    MAPK-IN-1
    		Inhibitor
    MAPK-IN-1 (Compound 2) is a MAPK signaling pathway inhibitor. MAPK-IN-1 exhibits AChE inhibitory activity with an IC50 of 23.84 μM. MAPK-IN-1 shows anti-neuroinflammatory and neuroprotective activity and can be used for Alzheimer's disease research.
    MAPK-IN-1
  • HY-110207
    SM-324405
    		Agonist 98.52%
    SM-324405 is a TLR7 agonistic antedrug (EC50 = 50 nM), with pEC50 values of 7.3 and 6.6 for human TLR7 and Rat TLR7, respectively. SM-324405 is used for immunoresearch of allergic diseases. An antedrug is defined as a locally active compound that is designed to be rapidly metabolized to an inactive form upon entry into the circulation and prevents systemic toxicity by losing its agonistic activity in a plasmatic environment.
    SM-324405
  • HY-148338
    TLR8 agonist 5
    		Agonist
    TLR8 agonist 5 is a potent TLR8 agonist with an EC50 value of 20 nM for HEK-Blue hTLR8. TLR8 agonist 5 activates the immune response.
    TLR8 agonist 5
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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