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-160230
    ssRNA41 sodium
    		Chemical
    ssRNA41 sodium is a 20-mer phosphothioate protected single-stranded RNA oligonucleotide. It derives from ssRNA40 by replacement of all U nucleotides with adenosine. ssRNA41 sodium is unable to induce the production of type IFNs, and therefore can be used as a negative control for ssRNA40.
    ssRNA41 sodium
  • HY-P2036
    FSL-1
    		Agonist 99.22%
    FSL-1, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection.
    FSL-1
  • HY-N7088R
    Raffinose (Standard)
    		Inhibitor
    Raffinose (Standard) is the analytical standard of Raffinose. This product is intended for research and analytical applications. Raffinose (Melitose) regulates intestinal flora, inhibits TLR4-MyD88-NF-κB signaling pathway, and activates Nrf2 signaling pathway. Raffinose exhibits anti-inflammatory, antioxidant, and immunomodulatory activities. Raffinose is orally active.
    Raffinose (Standard)
  • HY-123789
    T5342126
    		Antagonist 98.1%
    T-5342126 is a toll-like receptor 4 (TLR4) antagonist. It reduces LPS-induced production of nitric oxide (NO) in RAW 264.7 cells (IC50=27.8 μM), as well as decreases LPS-induced IL-8, TNF-α, and IL-6 production in isolated human whole blood (IC50s=110.5, 315.6, and 318.4 μM, respectively). T-5342126 (82 mg/kg) reduces ethanol intake and the abundance of ionized calcium-binding adapter molecule 1 (Iba1), a marker of microglial activation, in the central nucleus of the amygdala in ethanol-dependent mice.
    T5342126
  • HY-P11072
    IRF5-CPP5
    		Inhibitor
    IRF5-CPP5 is a cytosolic peptide that selectively inhibits human IRF5 with IC50 values of 15.4 and 15.3 μM for recombinant S430D or wild-type (WT) IRF5 dimerization, respectively..
    IRF5-CPP5
  • HY-N9347
    Stepharine
    		Inhibitor 98.0%
    Stepharine, an natural alkaloid, directly interactes with TLR4 and binds to the TLR4/MD2 complex (TLR4 inhibitor). Stepharine possesses anti-aging, anti-viral and anti-hypertensive effects.
    Stepharine
  • HY-P1180
    Pam3CSK4
    		Agonist
    Pam3CSK4 is a toll-like receptor 1/2 (TLR1/2) agonist with an EC50 of 0.47 ng/mL for human TLR1/2.
    Pam3CSK4
  • HY-D1056B2
    Lipopolysaccharides, from Proteus mirabilis
    Lipopolysaccharides, from Proteus mirabilis are lipopolysaccharide endotoxins and TLR-4 activators derived from Proteus mirabilis, 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 Proteus mirabilis exhibit a typical three-part structure: O-antigen, core oligosaccharide, and lipid A. Proteus mirabilis is a major pathogen causing urinary tract infections and may also contribute to rheumatoid arthritis. Lipopolysaccharides, from Proteus mirabilis also exhibit potential anti-tumor effects, demonstrating in vivo inhibitory activity against solid tumors such as meningosarcoma and Walker carcinosarcoma.
    It is recommended to prepare a solution with concentration ≥2 mg/mL. Vortex thoroughly for more than 10 minutes. Due to the adsorption characteristics of LPS, silanized container or low adsorption centrifuge tubes should be used for aliquoting and storage, and mix thoroughly before use.
    Lipopolysaccharides, from Proteus mirabilis
  • HY-153839A
    ODN 4084-F sodium
    		Inhibitor
    ODN 4084-F sodium is a class B (‘broadly-active’) inhibitory ODN. ODN 4084-F sodium is potent inhibitor of TLR9-induced B cells and macrophages.
    ODN 4084-F sodium
  • HY-145885
    TLR7/8 agonist 6
    		Agonist
    TLR7/8 agonist 6 (Compound 4) is the potent agonist of TLR7/8 with IC50s of 0.18 and 5.34 μM, respectively. TLR7/8 agonist 6 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for researching infectious disease, cancer, and autoimmune disorders.
    TLR7/8 agonist 6
  • HY-N14039
    Pinus pinaster bark extract
    		Activator
    Pinus pinaster bark extract is extracted from the bark of pine bark with antioxidant, anti-inflammatory and neuroprotective effects. Pinus pinaster bark extract increases toll-like receptor (TLR) activity, inducing production of IL-10.
    Pinus pinaster bark extract
  • HY-150744
    ODN 24888
    		Inhibitor
    ODN 24888 is an guanine-modified inhibitory oligonucleotides (INH-ODN), shows potent inhibition on TLR7/TLR9-mediated signaling. ODN 24888 impairs IFN-α level and NF-κB activation, inhibits IL-6 release. ODN 24888 involves in immune and inflammatory responses, can be used as a vaccine adjuvant.
    ODN 24888
  • HY-N3979
    Grossamide
    		Inhibitor 98.0%
    Grossamide is a natural product that can be isolated from fructus cannabis, the dried fruit of Cannabis sativa L.. Grossamide has anti-neuroinflammatory effects.
    Grossamide
  • HY-149650
    TLR4 agonist-1
    		Agonist
    TLR4 agonist-1 (compound 17a) is a potent agonist of Toll-like Receptor 4 (TLR4), and induces the generation of MIP-1β in RAW 264.7 and MM6 cells.
    TLR4 agonist-1
  • HY-165613
    Pam2Cys
    		Agonist
    Pam2Cys (Dipalmitoyl-S-glyceryl-cysteine; S-[2,3-Bis(palmitoyloxy)propyl]cysteine) is a selective agonist of dendritic cell TLR2, targeting the lipid portion of dendritic cells. Pam2Cys works by targeting and activating dendritic cells, thereby inducing strong immune responses, such as the production of specific antibodies. Pam2Cys enhances immunogenicity without the need for exogenous adjuvants. Pam2Cys can be applied to vaccine research, especially the development of lipopeptide vaccines against influenza A virus and other viruses to induce protective immune responses.
    Pam2Cys
  • HY-156693
    MTvkPABC-P5
    		Agonist
    MTvkPABC-P5d, a TLR7 agonist, is an immune stimulant. MTvkPABC-P5d can be used for synthesis of immune-stimulating antibody conjugates (ISACs).
    MTvkPABC-P5
  • HY-153543
    TLR7/8 agonist 8
    		Agonist 98.69%
    TLR7/8 agonist 8 (compound 24m) is a potent toll-like receptor 7/8 (TLR7/8) dual agonist, with EC50s of 27 and 12 nM for hTLR7 and hTLR8, respectively. TLR7/8 agonist 8 can improve the antitumor activity of PD-1/PD-L1 blockade.
    TLR7/8 agonist 8
  • HY-175222
    GlcNAc-MurNAc
    		Inhibitor
    GlcNAc-MurNAc, a disaccharide, is a TLR4 agonist with a Kd of 383 μM for murine TLR4. GlcNAc-MurNAc directly binds to TLR4 and activates its downstream NF-κB and IRF pathways. GlcNAc-MurNAc improves Dextran sulfate sodium salt (DSS) (HY-116282C)-induced colitis in mice through a TLR4-dependent mechanism. GlcNAc-MurNAc can be used for the study of inflammatory bowel disease.
    GlcNAc-MurNAc
  • HY-150501
    Diprovocim-X
    		Agonist 98.64%
    Diprovocim-X (compound 35) is a potent TLR1/TLR2 (toll-like receptor 1/2) agonist, with EC50 values of 0.14 and 0.75 nM for hTLR1/TLR2 and mTLR1/TLR2, respectively. Diprovocim-X is a potent adjuvant in vivo in mice, and serves to stimulate the adaptive immune response.
    Diprovocim-X
  • HY-176192
    SMU-14a
    		Inhibitor
    SMU-14a is a TLR3 inhibitor (IC50: 0.18 µM). SMU-14a inhibits IL-6 secretion in mouse peritoneal macrophages and downregulates TNF-α in human peripheral blood monocytes. SMU-14a exerts anti-inflammatory effects by reducing the phosphorylation of p65, ERK, and TBK1 through NF-κB, MAPK, and IRF3 signaling pathways, and decreasing serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels. SMU-14a can be used in the study of acute hepatitis.
    SMU-14a
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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