1. Signaling Pathways
  2. Immunology/Inflammation
  3. Toll-like Receptor (TLR)

Toll-like Receptor (TLR)

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-17003R
    Saquinavir mesylate (Standard)
    Inhibitor
    Saquinavir mesylate (Standard) (Ro 31-8959/003 (Standard)) is the analytical standard of Saquinavir mesylate (HY-17003). This product is intended for research and analytical applications. Saquinavir (Ro 31-8959) mesylate is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir mesylate also has anti-inflammatory activity and can induce apoptosis of human red blood cells.
    Saquinavir mesylate (Standard)
  • HY-156812
    SM-360320 drug-linker
    Agonist
    SM-360320 drug-linker (compound 19), a drug-linker of SM-360320 (HY-125390), is a small molecule immune agonist. SM-360320 drug-linker can be used to conjugated to PD-1 antibodies to form antibodies in resisting tumors.
    SM-360320 drug-linker
  • HY-179209
    TLR9-IN-2
    Inhibitor
    TLR9-IN-2 (Compound 20) is a selective inhibitor of Toll-like receptor 9 (TLR9) with IC50 values for TLR9, TLR7, and TLR8 of 25, 1400, and > 50,000 nM respectively. TLR9-IN-2 can be used for the study of fibrosis, autoimmune and inflammatory diseases.
    TLR9-IN-2
  • HY-163965
    Antitumor agent-185
    Antitumor agent-185 (compound 3) shows antitumor activity that could effectively reduce the growth of tumors and prolong the survival time of mice in vivo.
    Antitumor agent-185
  • HY-163829
    TLR2 agonist 1
    Agonist
    TLR2 agonist 1 (Compound R-7d) is an agonist for human toll-like receptor 2 (TLR 2) with an EC50 of 116 pM. TLR2 agonist 1 enhances NF-κB promoter activation through TLR2/TLR1 heterodimers.
    TLR2 agonist 1
  • HY-159916
    AYK004
    Agonist
    AYK004 is a TLR7/8 agonist that enhances immune responses by activating the TLR signaling pathway. AYK004 is an adenine derivative with a favorable hydrophilic-lipophilic balance, which improves the loading capacity and stability in immunoadjuvant systems such as liposomes, while reducing the side effects of the immunoadjuvant system in systemic immunity .
    AYK004
  • HY-146560
    Xanthine oxidase-IN-6
    Inhibitor
    Xanthine oxidase-IN-6 (Compound 6c) is a potent, orally active, mixed-type xanthine oxidase (XOD) inhibitor with an IC50 value of 1.37 µM. Xanthine oxidase-IN-6 shows strong anti-hyperuricemia and renal protective activity.
    Xanthine oxidase-IN-6
  • HY-N0741AR
    Leonurine hydrochloride (Standard)
    Leonurine (hydrochloride) (Standard) is the analytical standard of Leonurine (hydrochloride). This product is intended for research and analytical applications. Leonurine hydrochloride is an alkaloid isolated from Leonurus artemisia, with anti-oxidative and anti-inflammatory.
    Leonurine hydrochloride (Standard)
  • HY-150740
    ODN 21595
    Inhibitor
    ODN 21595 is a Guanine-Modified TLR7 and TLR9 inhibitor. ODN 21595 inhibits the release of IFN-α and IL-6 with no cytotoxic. ODN 21595 reduces the expression of CD86 and HLA-DR. ODN 21595 has the potential for the research of systemic lupus erythematosus (SLE).
    ODN 21595
  • HY-150212C
    Tilsotolimod sodium scrambled negative control
    Inhibitor
    Tilsotolimod sodium scrambled negative control is the sequence scrambled negative control of Tilsotolimod sodium.
    Tilsotolimod sodium scrambled negative control
  • HY-172934
    FGT-4
    Agonist
    FGT-4 is a folate receptor β (FR-β) targeting chimeric molecule. FGT-4 is a TLR7 agonist. FGT-4 facilitates the secretion of iNOS and proinflammatory cytokine IL-6 associated with M1 macrophages and enhances the proliferation of cytotoxic CD8+ T cells. FGT-4 has anti-tumor activity in the 4T1 breast cancer mouse model. FGT-4 can be used for the study of cancer immunity. (Pink: target protein TLR7/8 agonist 1 ligand (HY-103698); black: linker (HY-172936); blue: FR-β ligand (HY-172935)).
    FGT-4
  • HY-160228A
    ORN 02 sodium
    Activator
    ORN 02 (sodium) is a synthetic single-stranded U-rich RNA and contains 6 repeats of UUAU sequence motif. The AU-rich oligoribonucleotides (ORNs) are able to stimulate TLR8.
    ORN 02 sodium
  • HY-107272
    Chuanbeinone
    Inhibitor
    Chuanbeinone (22-Epidelavinone) is an orally active alkaloid found in Fritillaria pallidiflora. Chuanbeinone shows cytotoxicity against mutiple cancer cells and can induces apoptosis and S phase arrest. Chuanbeinone downregulates Bcl-2, upregulates Bax, and activates caspase-3. Chuanbeinone exerts anti-inflammatory and antitussive effects by reducing pro-inflammatory cytokine (IL-1β, IL-6 and TNF-α) production and mRNA expression, and inhibiting TRIF-, MyD88-, NF-κB-, and MAPK-dependent signaling pathways. Chuanbeinone inhibits AChE and BChE with IC50 values of 7.7 and 0.7 μM. Chuanbeinone can be used for the researches of lung carcinoma, cough, inflammatory diseases.
    Chuanbeinone
  • HY-121496
    3M-011
    Agonist
    3M-011 is a potent dual toll-like receptor TLR7/8 agonist and a cytokine inducer. 3M-011 significantly inhibits H3N2 influenza viral replication in the nasal cavity. 3M-011 is also a potent adjuvant to radiotherapy that induces local and profound systemic immune responses during radiotherapy. 3M-011 strongly has antitumor action.
    3M-011
  • HY-180336
    LM9
    Inhibitor
    LM9 is a potent, orally active MyD88 inhibitor. LM9 blocks TLR4/MyD88 binding, MyD88 homodimer formation, and TLR4/MyD88/NF-κB signaling pathway activation. LM9 prevents atherosclerosis by regulating inflammatory responses and oxidative stress in macrophages. LM9 efficiently mitigates inflammatory responses and fibrosis in obesity-induced cardiomyopathy. LM9 can be used for fibrosis and atherosclerosis research.
    LM9
  • HY-183573
    PTPRO-IN-1
    Inhibitor
    PTPRO-IN-1 is a selective, orally active PTPRO inhibitor with an IC50 of 0.16 μM. PTPRO-IN-1 exhibits IC50 values of 2.4 μM, 2.33 μM and 2.13 μM against PTPN22, PTP1B and PTPRT, respectively, and shows almost no inhibitory activity against STEP/SSH2. PTPRO-IN-1 inhibits the TLR4/NF-κB signaling pathway in macrophages, ameliorates colonic pathological conditions and suppresses the secretion of pro-inflammatory cytokines by T cells. PTPRO-IN-1 can be used for the research of inflammatory bowel disease.
    PTPRO-IN-1
  • HY-173129
    Anti-inflammatory agent 97
    Anti-inflammatory agent 97 (Compound 1l), an anti-inflammation agent, can also inhibit oxidative stress. Anti-inflammatory agent 97 can inhibit the colonic shortening and suppress inflammatory symptoms of the colonic tissue in the DSS (HY-116282C)-induced ulcerative colitis mice model. Anti-inflammatory agent 97 can regulate the inflammation-related TLR4/NF-κB signaling pathway and the oxidative stress-related Nrf2/HO-1 signaling pathway.
    Anti-inflammatory agent 97
  • HY-160938
    β-Funaltrexamine
    Inhibitor
    β-Funaltrexamine (β-FNA) is a blood-brain barrier-permeable, selective and irreversible μ-opioid receptor antagonist with immunomodulatory, anti-inflammatory and neuroprotective activities. β-Funaltrexamine inhibits p38 MAPK and TLR4 signaling by blocking μ-opioid receptors, and reduces the transcriptional activities of NF-κB, AP-1, CREB and Stat. Furthermore, β-Funaltrexamine inhibits iNOS activation and pro-inflammatory microglial polarization, converting microglia to an anti-inflammatory phenotype, thereby downregulating neuroinflammation and ameliorating neuronal degeneration. β-Funaltrexamine is widely applicable to research related to stroke, cerebral ischemia/reperfusion injury and neurodegenerative diseases.
    β-Funaltrexamine
  • HY-173079
    TLR7 agonist 30
    Agonist
    TLR7 agonist 30 (compound 2) is an agent-linker conjugate for ADC. TLR7 agonist 30 contains a TLR7 agonist (compound 1) and a cleavable linker, and has potent anti-tumor activity.
    TLR7 agonist 30
  • HY-N16009
    α-Rhamnosyl FP20 sodium
    α-Rhamnosyl FP20 sodium, a TLR-4 agonist, is a vaccine adjuvant.
    α-Rhamnosyl FP20 sodium
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