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-134581
    Enpatoran
    		Inhibitor 99.80%
    Enpatoran (M5049) is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran exhibits excellent pharmacokinetic properties in vivo. Enpatoran can be used for both innate and adaptive autoimmunity blocking research .
    Enpatoran
  • HY-108473
    CU-CPT 4a
    		Inhibitor 99.50%
    CU-CPT 4a (TLR3-IN-1) is a potent, highly selective TLR3 signaling inhibitor. CU-CPT 4a represses the expression of downstream signaling pathways mediated by the TLR3/dsRNA complex, including TNF-α and IL-1β.
    CU-CPT 4a
  • HY-108910
    Chymotrypsin
    		Inhibitor
    Chymotrypsin (EC 3.4.21.1; Chymotrypsin A) is an orally effective inhibitor targeting molecules such as TLR4, NF-κB, MMP-1, TNF-α, IL-1β, and IL-6. Chymotrypsin downregulates the TLR4/NF-κB signaling pathway, inhibiting the release of inflammatory factors, reducing cell infiltration and tissue damage. It also reduces the expression of tumor cell adhesion molecules (such as CD44 and CD54) and can be specifically detected by fluorescent probes (such as NBD-3). Chymotrypsin has anti-inflammatory, hepatoprotective, joint damage-reducing, liver protection against lipotoxicity, and anti-tumor metastasis functions. It can be used in research on diseases such as rheumatoid arthritis, non-alcoholic fatty liver disease, and melanoma metastasis. Chymotrypsin can be used in studies of inflammation, edema, and expectoration.
    Chymotrypsin
  • HY-P9930
    Evolocumab
    		Inhibitor 98.40%
    Evolocumab (AMG 145) is a human monoclonal antibody that inhibits PCSK9. Evolocumab is used in the study of hypercholesterolemia and atherosclerotic cardiovascular disease. Evolocumab binds to circulating PCSK9 protein and inhibits its binding to LDLR. Evolocumab has antioxidant and cytoprotective activities against H2O2-induced oxidative damage to endothelial cells. Evolocumab may also negatively regulate activation of the TLR-4/NF-κB signaling pathway to prevent inflammation.
    Evolocumab
  • HY-146244
    Agatolimod
    		Agonist 98.84%
    Agatolimod ((ODN 2006; PF-3512676; CpG 7909)) is a TLR9 agonist and immunomodulator with an EC50 of 180 nM against human TLR9. Agatolimod activates and upregulates the expression of both TLR9 and TLR6, and mediates downstream signaling pathways via IRAK4, IRF5, IRF7. Agatolimod induces Th1-type innate and adaptive immune responses, activates various immune cells and promotes antigen presentation, regulates antibody levels and immune cell infiltration, upregulates the secretion of multiple cytokines, induces apoptosis and cell cycle arrest, enhances cytotoxicity, and clears intracellular Salmonella. Agatolimod is applicable to research on COVID-19, breast cancer, lung adenocarcinoma, HPV-related tumors, melanoma, and salmonellosis.
    Agatolimod
  • HY-149652
    IRF5-IN-1
    		Inhibitor 99.91%
    IRF5-IN-1 (Compound C5) is a conformationally locked inhibitor for SLC15A4. IRF5-IN-1 blocks the downstream IRF5 activation, inhibits the TLR7/8 signaling pathway. IRF5-IN-1 exhibits anti-inflammatory responses.
    IRF5-IN-1
  • HY-108471
    CU-CPT22
    		Inhibitor ≥99.0%
    CU-CPT22 is a potent protein complex of toll-like receptor 1 and 2 (TLR1/2) inhibitor, and competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with a Ki of 0.41 µM. CU-CPT22 blocks Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 µM.
    CU-CPT22
  • HY-17007
    Saquinavir
    		Inhibitor 99.77%
    Saquinavir (Ro 31-8959) is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir also has anti-inflammatory activity and can induce apoptosis of human red blood cells.
    Saquinavir
  • HY-N0680
    Thiamine hydrochloride
    		Inhibitor 99.97%
    Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.Thiamine hydrochloride activates NrF-2/HO-1 and inhibits TLR4, NF-κB. Thiamine hydrochloride has neuroprotective and anti-inflammatory effects. Thiamine hydrochloride can be used in the studys of diabetic complications, neurological diseases, cancers, and colitis.
    Thiamine hydrochloride
  • HY-139567
    Afimetoran
    		Antagonist 99.37%
    Afimetoran (BMS-986256) is an orally active, selective, and highly bioavailable TLR7/8 antagonist. Afimetoran (BMS-986256) can inhibit TLR7/8 activation of the NF-κB pathway and reverse TLR7 mediated resistance to steroid induced apoptosis in plasma cell like dendritic cells (pDCs). Afimetoran (BMS-986256) can be used for research on inflammation and autoimmune diseases (systemic lupus erythematosus).
    Afimetoran
  • HY-123942
    Diprovocim
    		Agonist 98.82%
    Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC50=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses.
    Diprovocim
  • HY-W250113
    Zymosan A
    		Agonist
    Zymosan A (Zymosan A from Saccharomyces cerevisiae) is a TLR2 agonist, that targeting TLRs can prevent and suppress IR-induced intestinal injury. Zymosan A exhibits a significant radioprotective effect, and protects IR-induced intestinal injury in mice. Zymosan A promotes the regeneration of intestinal stem cells (ISCs), after IR injury.
    Zymosan A
  • HY-107575
    TLR4-IN-C34
    		Inhibitor 99.94%
    TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.
    TLR4-IN-C34
  • HY-129522
    Sulfo-ara-F-NMN
    		Activator 99.36%
    Sulfo-ara-F-NMN (CZ-48) is a mimetic of nicotinamide mononucleotide (NMN). Sulfo-ara-F-NMN acts selectively, activating SARM1 but inhibiting CD38 (IC50 around 10 μM). Sulfo-ara-F-NMN induces intracellular cyclic ADP-ribose (cADPR) production.
    Sulfo-ara-F-NMN
  • HY-W021879
    DSRM-3716
    		Inhibitor 99.91%
    DSRM-3716 (5-Iodoisoquinoline) is a potent and selective SARM1 NADase inhibitor with an IC50 of 75 nM. DSRM-3716 is selective against other NAD+-processing enzymes, receptors, and transporters. DSRM-3716 provides robust axon protection.
    DSRM-3716
  • HY-150741C
    ODN 2216 sodium
    		Agonist 98.57%
    ODN 2216 sodium is a type A CpG oligodeoxynucleotide vaccine adjuvant and a TLR9 agonist. ODN 2216 sodium interacts with TLR9 in the lysosomes of CD4+ T cells and activates feedback-dependent signaling pathways. ODN 2216 sodium induces the production of type I interferons, IL-6 and TGF-β via the IRAK4/IRF7 axis, while increasing intracellular ATP levels. ODN 2216 sodium not only induces the differentiation of CD4+ T cells into anti-inflammatory Th3-like regulatory phenotypes to inhibit autologous proliferation, but also enhances the specific CD8+ T cell-mediated cytotoxicity against Mammaglobin-A in breast cancer cells. ODN 2216 sodium is widely used in studies related to breast cancer and systemic lupus erythematosus.
    ODN 2216 sodium
  • HY-147295
    Odetiglucan
    		Agonist
    Odetiglucan is a novel β-glucan that is a potent immunostimulant and a Dectin-1 (CLEC7A) agonist. Odetiglucan activates innate immune effector cells and triggers a coordinated anti-cancer immune response.
    Odetiglucan
  • HY-B0180A
    Imiquimod hydrochloride
    		Agonist 99.77%
    Imiquimod hydrochloride (R 837 hydrochloride), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod hydrochloride exhibits antiviral and antitumor effects in vivo. Imiquimod hydrochloride can be used for the research of external genital, perianal warts, cancer and COVID-19.
    Imiquimod hydrochloride
  • HY-150724C
    ODN 1018 sodium
    		Agonist
    ODN 1018 (1018 ISS) sodium is a TLR9 agonist and immune modulator. ODN 1018 sodium exhibits adjuvant activity and augments CD8+ T cell responses with LNP-encapsulated OVA peptides. ODN 1018 sodium triggers sustained suppression of allergic airway inflammation. ODN 1018 sodium can be used for the research of allergic asthma and systemic lupus erythematosus.
    ODN 1018 sodium
  • HY-131166
    Curdlan
    		Activator 98.5%
    Curdlan is a polysaccharide found in bacteria, consisting of a glucose homopolymer with β-1,3-glycosidic linkages. Curdlan can be recognized by Dectin-1 (a C-type lectin receptor), inducing immune responses in tissue mast cells and enhancing dendritic cell effects in tumor immunity. Curdlan holds potential for research in cancer and immune-inflammatory diseases.
    Curdlan
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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