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-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-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-153071
    TLR7 agonist 6
    		Agonist 98.08%
    TLR7 agonist 6 (compound IIb-19) is an TLR7 agonist with an EC50 value of 1.0 nM.
    TLR7 agonist 6
  • HY-150729
    ODN 1982
    		Inhibitor
    ODN 1982 is a unmethylated oligodeoxyribonucleotide (ODN) with no CpG motif, can be used to prepare DNA vaccines. ODN 1982 inhibits R-848 signaling. ODN 1982 sequence: 5’-tccaggacttctctcaggtt-3’.
    ODN 1982
  • 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-182500A
    (S,S)-SARM1-IN-9
    		Inhibitor 99.67%
    (S,S)-SARM1-IN-9 (Compound MY-13A) is a stereoselective SARM1 inhibitor with covalent binding properties. (S,S)-SARM1-IN-9 covalently modifies Cys311 in the autoregulatory ARM domain of wild-type SARM1, thereby blocking NADase activity, without inhibiting the SARM1C311A or SARM1C311S mutants. (S,S)-SARM1-IN-9 blocks vacor- and vincristine-induced axon degeneration in primary rodent dorsal root ganglion neurons. (S,S)-SARM1-IN-9 can be used for research on axon degeneration-dependent neurological disorders, including chemotherapy-induced peripheral neuropathy.
    (S,S)-SARM1-IN-9
  • 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-P1405A
    Pam3CSK4-Biotin TFA
    		Agonist 98.02%
    Pam3CSK4-Biotin (Pam3Cys-Ser-(Lys)4-Biotin) TFA is biotinylated Pam3CSK4. Pam3CSK4-Biotin TFA is a Toll-like receptor 1/2 (TLR1/2) agonist.
    Pam3CSK4-Biotin TFA
  • HY-N12378
    β-Patchoulene
    		Inhibitor
    β-Patchoulene is an orally active anti-inflammatory, antioxidant, and anti-apoptotic agent. β-Patchoulene inhibits the NF-κB, TLR4, and cAMP/PKA/CREB signaling pathways; activates the Sirt1/Nrf2 and AMPK signaling pathways; and targets Fas/FasL, Caspase-3, ERK1/2, ROCK1/MLC2 for inhibition. β-Patchoulene regulates cytokine secretion, inflammatory cell infiltration, lipid peroxidation, cell polarization, gut microbiota, and lipid metabolism, restores barrier function, mitochondrial function, and cell viability, and exhibits repellent activity against Spodoptera exigua larvae. β-Patchoulene can be used in research related to various inflammatory, ischemic, fibrosis-associated diseases, as well as hepatocellular carcinoma.
    β-Patchoulene
  • HY-P11003
    PTD-N5-1
    		Inhibitor
    PTD-N5-1 (N5-1) is an IRF5 inhibitory peptide. PTD-N5-1 blocks β-glucan-induced IL-12 production in IFN-γ primed wild-type and Clec2d-difecient bone-marrow-derived dendritic cells (BMDCs). PTD-N5-1 regulates antifungal immunity through suppression of IRF5-mediated IL-12 production.
    PTD-N5-1
  • HY-162649
    TIC10g
    		Inhibitor 98.92%
    TIC10g is a dual inhibitor for toll-like receptor 7 and 9 (TLR7 and TLR9), which inhibits TLR7 and TLR9 mediated TNF-α release in mouse macrophages (IC50 is 14.5 μM and 6.5 μM) and human B lymphocytes (IC50 is 7.69 μM and 11.5 μM). TIC10g inhibits the activation of NF-κB and MAPK, and exhibits anti-inflammatory activity against systemic lupus erythematosus and rheumatoid arthritis .
    TIC10g
  • 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-17589S1
    Chloroquine-d4 phosphate
    		Inhibitor 98.01%
    Chloroquine-d4 (phosphate) is the deuterium labeled Chloroquine phosphate. Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
    Chloroquine-d<sub>4</sub> phosphate
  • HY-182644
    SMU-Z1
    		Agonist
    SMU-Z1 is a TLR1/2 heterodimer agonist with an EC50 of 4.88 nM. SMU-Z1 activates the NF-κB pathway, triggers pro-inflammatory cytokine production, and induces the generation of TNF-α, IL-1β, IL-6 and NO. SMU-Z1 promotes splenocyte proliferation and upregulates the expression of CD8+T cells, NK cells and dendritic cells. SMU-Z1 exhibits significant anti-tumor effects in mouse leukemia models. SMU-Z1 can be used for leukemia-related research.
    SMU-Z1
  • HY-150212
    Tilsotolimod
    		Inhibitor 99.46%
    Tilsotolimod (IMO-2125) is a TLR9 agonist. Tilsotolimod activates the TLR9 signaling pathway, triggers downstream pro-inflammatory and immunostimulatory pathways, enhances the uptake and killing of cancer cells, and induces adaptive immune responses. Tilsotolimod is applicable to research related to melanoma and colorectal cancer.
    Tilsotolimod
  • HY-N7700
    Guluronic acid
    		Inhibitor 98.90%
    Guluronic acid (G2013) is an orally active oxidative stress regulator and anti-inflammatory agent that exerts pharmacological effects by down-regulating various pro-inflammatory and oxidative stress-related genes (such as TLR4, NF-κB, iNOS, etc.) and inhibiting the activities of COX-2, MMPs and VEGF. Low-dose Guluronic acid up-regulates the expression of immunoregulatory genes SHIP1 and SOCS1, thereby effectively inhibiting cancer-related inflammation, tumor angiogenesis, cell adhesion and metastasis, while reducing the accumulation of immunosuppressive cells. Guluronic acid significantly prolongs the survival time of tumor-bearing hosts within a concentration range without direct cytotoxicity, demonstrating favorable safety. Guluronic acid has involved in the research of multiple sclerosis, ankylosing spondylitis, breast cancer and other inflammatory diseases.
    Guluronic acid
  • 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-179474
    TSI-13-57
    		Inhibitor 98.73%
    TSI-13-57 is a pan-TLR inhibitor (IC50: 2.7 μM, 6.03 μM, 7.37 μM, 6.38 μM for TLR9, TLR7, TLR2, TLR4, respectively). TSI-13-57 inhibits homodimerization of the TIR domains of MyD88. TSI-13-57 reduces systemic inflammatory responses in LPS-induced mice.
    TSI-13-57
  • HY-176192
    SMU-14a
    		Inhibitor
    SMU-14a is a selective Toll-like receptor 3 (TLR3) inhibitor wirh an IC50 of 0.18 μM. SMU-14a reduces phosphorylation of p65, ERK, and TBK1 via NF-κB, MAPK, and IRF3 signaling pathways. SMU-14a inhibits IL-6 secretion in mouse peritoneal macrophages, downregulates TNF-α in human peripheral blood monocytes and decreases serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels. SMU-14a can be used for the research 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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