Toll-like Receptors

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  1. D18

    TLR7/8 Agonist

    D18 is a dual agonist for Toll-like receptors 7 and 8 (TLR7/8), exhibiting EC50 values of 24 nM and 10 nM, respectively. This immune modulator enhances PD-L1 expression through epigenetic mechanisms, thereby increasing tumor sensitivity to PD-1/PD-L1 blockade. D18 demonstrates significant immune activation and anti-tumor effects, making it valuable in cancer research, including studies focused on colon cancer. Additionally, D18 serves as a cytotoxin for the synthesis of antibody-drug conjugate HE-S2.
  2. TLR7/8 Agonist

    AXC-715 hydrochloride is a dual agonist targeting TLR7 and TLR8. It demonstrates significant immunomodulatory activity, making it a valuable tool in the development of antibody-adjuvant immunoconjugates. This compound can be utilized to enhance the efficacy of therapies targeting programmed death-ligand 1 (PD-L1) by linking it to one or more adjuvants, advancing research in cancer immunotherapy and immune response modulation.
  3. TLR4/NF-κB Inhibitor

    TLR4/NF-κB-IN-1 is a selective inhibitor of the TLR4/NF-κB signaling pathway, demonstrating significant anti-inflammatory properties. This compound exhibits the ability to penetrate the blood-brain barrier, making it suitable for studies involving neuroinflammation. In murine models, TLR4/NF-κB-IN-1 effectively reduces acute neuroinflammation induced by lipopolysaccharides (LPS) while downregulating the expression of TLR4, phosphorylated NF-κB, and phosphorylated IκB-α proteins, providing a valuable tool for researching neuroinflammatory processes and their therapeutic modulation.
  4. TLR8 Antagonist

    TLR8 antagonist-1 is a selective antagonist targeting Toll-like receptor 8 (TLR8). It effectively inhibits TLR8-mediated inflammatory responses and associated signaling pathways, including the recruitment of MyD88 and the activation of NF-κB and IRF pathways. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for research in inflammation and immune response modulation.
  5. TLR7 Agonist

    BNT411 is a selective TLR7 agonist known for its ability to stimulate the production of interferon-alpha (IFNa) both in vivo and in vitro. This compound exhibits anticancer properties, making it a valuable tool in cancer research, particularly for non-small cell lung cancer, pancreatic cancer, and untreated extensive-stage small cell lung cancer (ES-SCLC). Its mechanism of action and efficacy in activating immune responses make it a key reagent for investigating cancer immunotherapy.
  6. TLR7/8 Antagonist

    TLR7/8 antagonist 2 is a potent antagonist specifically targeting Toll-like receptors 7 and 8, with IC50 values of 4.9 nM and 0.6 nM, respectively. This compound is essential for studying the role of TLR7 and TLR8 in autoimmune diseases, such as systemic lupus erythematosus, where their inappropriate activation contributes to pathogenesis. TLR7/8 antagonist 2 holds significant potential for advancing research in the field of autoimmune disorders.
  7. TLR7/8 Agonist

    TLR7/8 Agonist 6 is a potent agonist of Toll-like receptors 7 and 8, exhibiting IC50 values of 0.18 μM and 5.34 μM, respectively. As an imidazoquinoline derivative, this compound plays a crucial role in enhancing immune responses. It is particularly valuable in the investigation of immunomodulatory therapies for infectious diseases, cancer, and autoimmune disorders.
  8. TLR9 Agonist

    ODN D-SL01 is a class B CpG oligodeoxynucleotide that acts as a TLR9 agonist. It exhibits potent immunostimulatory properties in various vertebrate species and demonstrates anticancer activity. The specific sequence of ODN D-SL01 is 5'- T-C-G-C-G-A-C-G-T-T-C-G-C-C-C-G-A-C-G-T-T-C-G-G-T-A-3'. This compound is valuable for research applications focused on immune modulation and cancer therapy.
  9. TLR7 Agonist

    SM-276001 is a potent selective TLR7 agonist known for its ability to induce antitumor immune responses. This compound acts as an orally active interferon inducer, enhancing the body’s immune system to target and combat tumor cells. It is particularly useful in cancer research and immunotherapy studies aimed at understanding TLR7-mediated pathways in the immune response.
  10. TLR4 Inhibitor

    M62812 is a selective toll-like receptor 4 (TLR4) inhibitor that attenuates endothelial and leukocyte activation. By inhibiting TLR4 signaling, M62812 effectively diminishes LPS-induced coagulation and inflammatory responses, offering protective effects against lethal septic shock in murine models. This reagent serves as a valuable tool for research focused on the mechanisms of sepsis and related inflammatory disorders.
  11. TLR4 Agonist

    GSK1795091 is a synthetic TLR4 agonist that serves as a potent immunologic stimulator. It demonstrates significant antitumor activity by inhibiting tumor growth and enhancing survival in murine models. Additionally, GSK1795091 acts as an effective vaccine adjuvant, improving both mucosal and systemic immune responses to influenza virus vaccines, and has been shown to promote long-term survival in influenza challenge models. This compound is valuable for research applications in immunology and cancer therapeutics.
  12. TLR7 Agonist

    Ruzotolimod is an orally active TLR7 agonist that demonstrates potent antiviral effects by inhibiting viral replication of the Woodchuck hepatitis virus (WHV). Additionally, in combination with RO-7049389, it effectively reduces AAV-HBV viral load. This compound is valuable for research applications involving viral infections, including studies on COVID-19 or SARS-CoV-2.
  13. TLR7/8/9 Antagonist

    TLR7/8/9 Antagonist 2 is a potent orally active inhibitor targeting Toll-like receptors 7, 8, and 9. It demonstrates significant inhibitory effects on HEK/hTLR7, HEK/hTLR8, and HEK/hTLR9, with IC50 values of 0.011 μM, 0.029 μM, and 0.052 μM, respectively. This compound exhibits high bioavailability in vivo, making it a valuable tool for investigating auto-inflammatory diseases, including systemic lupus erythematosus and lupus nephritis.
  14. TLR 8 Agonist

    CU-CPD107 is a selective toll-like receptor 8 (TLR 8) agonist that modulates TLR 8 signaling pathways. This compound enhances immune responses when co-administered with single-stranded RNA (ssRNA), leading to synergistic activation of TLR 8. Additionally, CU-CPD107 suppresses the expression of pro-inflammatory factors, mitigating unwanted immune responses in the presence of ssRNA. This reagent is valuable for research into TLR 8's role in immune modulation and inflammation.
  15. Toll-like Receptor (TLR) Antagonist

    T5342126 is a potent antagonist of Toll-like receptor 4 (TLR4), designed to modulate immune responses. It effectively inhibits lipopolysaccharide (LPS)-induced nitric oxide production in RAW 264.7 cells, with an IC50 of 27.8 μM. Additionally, T5342126 reduces LPS-induced production of pro-inflammatory cytokines, including IL-8, TNF-α, and IL-6 in isolated human whole blood, with IC50 values of 110.5 μM, 315.6 μM, and 318.4 μM, respectively. In vivo, T5342126 (82 mg/kg) decreases ethanol consumption and mitigates microglial activation, as indicated by reduced Iba1 levels, in the central nucleus of the amygdala of ethanol-dependent mice, highlighting its potential in neurological research.
  16. TLR9 Agonists

    ODN 2336 is a potent TLR9 agonist classified as an A-Class CpG oligodeoxynucleotide (ODN). It effectively stimulates the production of interferon-alpha (IFN-α) and upregulates the expression of IP-10 and IL-18 mRNA. ODN 2336 serves as a valuable adjuvant in vaccine development and research, enhancing immune responses and providing insights into nucleic acid-based immunotherapy.
  17. TLR2 Agonist

    Pam2Cys is a TLR2 agonist that acts as an immunostimulant by binding to TLR2, activating dendritic cells, and initiating the TLR2-dependent NF-κB signaling pathway. This compound promotes dendritic cell maturation through the upregulation of MHC II molecules, enhances innate immune signaling, and drives pro-inflammatory responses, including the release of IL-12 and other cytokines. Additionally, Pam2Cys serves as a lipid moiety in synthetic lipopeptide vaccines, boosting immunogenicity, while selectively inducing pro-inflammatory macrophage activation. Research applications include studies on tuberculosis and influenza A virus infections, as it effectively recruits immune cells and mitigates infection-related symptoms without compromising adaptive immunity.
  18. TLR7/8 Agonist

    INI-4001 is a TLR7/8 agonist that modulates innate and adaptive immune responses by activating both murine TLR7 and human TLR7/TLR8 pathways. This compound enhances immunological responses, leading to increased IgG and neutralizing antibodies against Powassan virus (POWV) while concurrently reducing viral loads in multiple organs, including the brain and liver. INI-4001 also provides complete protection from lethal POWV challenges and promotes a Th1-biased immune response. It has demonstrated efficacy when used in combination with aluminum hydroxide and SARS-CoV-2 RBD antigen, making it valuable for research on Powassan virus infection and COVID-19 immunology.
  19. TLR7 Agonist

    TLR7 Agonist 4 is a potent TLR7 agonist, exhibiting an EC50 of 4.3 nM. This compound activates TLR7, a key receptor in the innate immune response, facilitating the advancement of research in immunology and inflammatory diseases. Its specific biological activity makes it suitable for studies involving viral infections, autoimmunity, and cancer therapy applications.
  20. TLR4/MyD88/NF-κB Inhibitor

    SjDX5-271 is a small peptide inhibitor targeting the TLR4/MyD88/NF-κB signaling pathway. It is known to induce cell polarization and mitigate hepatic inflammation, demonstrating protective effects against liver ischemia-reperfusion injury in mouse models. This compound is valuable for research in immunology and liver-related inflammation studies.
  21. TLR4 Antagonist

    Eritoran tetrasodium is a Toll-like receptor 4 (TLR4) antagonist with notable anti-inflammatory properties. It has demonstrated the ability to protect against lethal infections caused by viruses such as influenza, Ebola virus (EBOV), and Marburg virus (MARV). By decreasing granulocytosis, Eritoran tetrasodium may also alleviate the severity associated with cytokine storms. The compound plays a significant role in inhibiting the pathogenesis of filovirus infections, making it valuable for research applications in virology and immunology.
  22. TLR9 Inhibitor

    ODN 21158 is a selective inhibitor of Toll-like receptors 3 (TLR3) and 9 (TLR9). It effectively reduces interferon-alpha (IFN-α) secretion in a dose-dependent manner without exhibiting cytotoxic effects. This reagent is valuable for research applications involving immune modulation and the study of innate immune responses.
  23. TLR2-TLR1 Agonist

    a15:0-i15:0 PE is a diacyl phosphatidylethanolamine that functions as a non-canonical agonist for the TLR2-TLR1 heterodimer. It exhibits significant immunogenic activity, activating both T cells and dendritic cell signaling pathways while also demonstrating anti-inflammatory properties. a15:0-i15:0 PE promotes the production of pro-inflammatory cytokines such as TNFα and IL-6 and constitutes approximately 50% of the lipid membrane in A. muciniphila, highlighting its biological relevance in microbiome studies and immune response research.
  24. Toll-like Receptor (TLR) Agonist

    Vidutolimod (CMP-001) is a CpG-A oligodeoxynucleotide that acts as a Toll-like receptor 9 (TLR9) agonist. It effectively activates plasmacytoid dendritic cells (pDCs), resulting in the release of interferon alpha (IFNα). This mechanism initiates a series of anti-tumor immune responses, making Vidutolimod a valuable tool for cancer immunotherapy research and the study of immune modulation.
  25. TLR3 inhibitor

    SMU-CX1 is a selective TLR3 inhibitor with an IC50 of 0.11 μM, demonstrating effective inhibition across various influenza A virus subtypes, with IC50 values ranging from 0.14 to 0.33 μM. Additionally, SMU-CX1 shows antiviral activity against SARS-CoV-2, targeting viral PB2 and NP proteins with an IC50 of 0.43 μM. Furthermore, SMU-CX1 modulates the inflammatory response in host cells by inhibiting key factors such as IFN-β, IP-10, and CCL-5, making it a valuable tool for research in virology and innate immune response.
  26. TLR4 Inhibitor

    Stepharine is a natural alkaloid that functions as a toll-like receptor 4 (TLR4) inhibitor by directly interacting with the TLR4/MD2 complex. This compound exhibits significant biological activities, including anti-aging, anti-viral, and anti-hypertensive effects. It is of value in research applications focused on immune modulation and the treatment of inflammatory diseases.
  27. TLR Ligand

    ODN 2007 is a class B CpG oligodeoxynucleotide (ODN) that functions as a Toll-like receptor (TLR) ligand. This compound serves as an effective immunomodulator and vaccine adjuvant, enhancing immune responses across a range of species, including mammals, fish, and humans. Its specific sequence is 5'-TCGTCGTTGTCGTTTTGTCGTT-3', making it a valuable tool for research applications in immunology and vaccine development.
  28. TLR1/2 Agonist

    Pam3CSK4 is a potent agonist of toll-like receptors 1 and 2 (TLR1/2), exhibiting an EC50 of 0.47 ng/mL for human TLR1/2 activation. This compound is instrumental in stimulating innate immune responses, making it a valuable tool for research in immunology and related fields. Its application is pivotal in studies aimed at understanding pathogen recognition and the subsequent activation of immune pathways.
  29. TLR7/TLR9 Inhibitor

    ODN 24888 is a guanine-modified inhibitory oligonucleotide (INH-ODN) that specifically targets TLR7 and TLR9 signaling pathways. It effectively inhibits interferon-alpha (IFN-α) secretion and NF-κB activation, while also reducing interleukin-6 (IL-6) release. ODN 24888 is valuable for studying immune and inflammatory responses and can be utilized as a vaccine adjuvant in various research applications.
  30. TLR7 Agonist

    TLR7 Agonist 6 is a potent TLR7 activator with an EC50 value of 1.0 nM. This compound modulates immune responses by activating Toll-like receptor 7, which is crucial for recognizing viral RNA and activating downstream signaling pathways. TLR7 Agonist 6 is valuable for research in immunology, particularly in studies exploring antiviral responses and the development of therapeutic strategies for infectious diseases.
  31. TLR4 Agonist

    TLR4 agonist-1 is a potent Toll-like Receptor 4 (TLR4) agonist that effectively stimulates the immune response. It has been shown to induce the production of MIP-1β in RAW 264.7 and MM6 cell lines. This compound is valuable for research into innate immunity and the modulation of inflammatory processes.
  32. TLR Inhibitor

    TIC10g is a dual inhibitor of toll-like receptors 7 and 9 (TLR7 and TLR9). It effectively decreases TNF-α release in mouse macrophages and human B lymphocytes, with IC50 values of 14.5 μM and 6.5 μM for TLR7, and 7.69 μM and 11.5 μM for TLR9, respectively. TIC10g also inhibits the activation of NF-κB and MAPK pathways, demonstrating potential as an anti-inflammatory agent in conditions such as systemic lupus erythematosus and rheumatoid arthritis.
  33. TLR7 Agonist

    MTvkPABC-P5 is a toll-like receptor 7 (TLR7) agonist that serves as an immune stimulant. This compound can be utilized in the synthesis of immune-stimulating antibody conjugates (ISACs), making it valuable for research applications focused on enhancing immune responses. Its ability to activate TLR7 positions MTvkPABC-P5 as an important reagent in immunological studies and therapeutic development.
  34. TLR7/8 Dual Agonist

    TLR7/8 Agonist 8 is a potent dual agonist for toll-like receptors 7 and 8, demonstrating EC50 values of 27 nM and 12 nM for human TLR7 and TLR8, respectively. This compound enhances antitumor activity in combination with PD-1/PD-L1 blockade, making it a valuable tool for cancer immunotherapy research. Its ability to activate these key immune receptors positions TLR7/8 Agonist 8 as an important reagent in the study of immune modulation and tumor microenvironment interactions.
  35. TLR1/TLR2 Agonist

    Diprovocim-X is a highly effective agonist of toll-like receptors 1 and 2 (TLR1/TLR2), exhibiting EC50 values of 0.14 nM for human TLR1/TLR2 and 0.75 nM for mouse TLR1/TLR2. This compound functions as a potent immunological adjuvant in vivo, effectively enhancing the adaptive immune response in murine models. Diprovocim-X is suitable for research applications related to immunotherapy and vaccine development, facilitating the study of immune modulation.
  36. Pan-TLR Inhibitor

    TSI-13-57 is a pan-toll-like receptor (TLR) inhibitor that effectively targets TLR9, TLR7, TLR2, and TLR4 with IC50 values of 2.7 μM, 6.03 μM, 7.37 μM, and 6.38 μM, respectively. It functions by inhibiting the homodimerization of the TIR domains within the MyD88 pathway, thereby modulating immune responses. TSI-13-57 has been shown to significantly reduce systemic inflammatory responses in LPS-induced murine models, making it a valuable tool for research in inflammation and immune signaling pathways.
  37. TLR7 Ligand

    TMX-201 is a TLR7 ligand-phospholipid conjugate that functions as a potent immune stimulator. Its activity enhances immune responses, making it a valuable tool in cancer research, particularly in studies of breast cancer and melanoma. TMX-201 is useful for exploring TLR7-mediated pathways and their implications in tumor immunology.
  38. TLR4 Agonist

    Monophosphoryl Lipid A-12 (MPLA-12) is a potent agonist of Toll-like receptor 4 (TLR4). It exhibits important biological activity in modulating immune responses, making it a valuable tool for immunization studies and vaccine research. Its ability to stimulate TLR4 signaling cascades positions MPLA-12 as a key compound for investigating immune system activation and potential therapeutic applications in infectious diseases and cancer vaccines.
  39. TLR4 Signaling Inhibitor

    NCI126224 is a TLR4 signaling inhibitor that modulates immune responses by suppressing lipopolysaccharide (LPS)-induced production of key inflammatory mediators, including NF-κB, TNF-α, IL-1β, and nitric oxide. This compound demonstrates biological activity in the low nanomolar to low micromolar range, making it a valuable tool for research into inflammatory diseases and their mechanisms. Its ability to interfere with TLR4 signaling pathways positions NCI126224 as a significant reagent for exploring potential therapeutic strategies in inflammation-related studies.
  40. Toll-like Receptor (TLR) Inhibitor

    Cavrotolimod is a Toll-like Receptor 9 (TLR9) agonist that enhances immune responses through its structure as a spherical nucleic acid (SNA) modified with type B CpG oligonucleotides. This compound plays a crucial role in oncology research by stimulating the immune system, potentially leading to improved anti-tumor activity. Its application in cancer immunotherapy positions Cavrotolimod as a valuable research tool for understanding immune mechanisms and developing novel therapeutic strategies.
  41. Toll-like Receptor (TLR) Agonist

    Polvitolimod is a Toll-like Receptor 7 (TLR7) agonist that plays a crucial role in immune response modulation. This compound is primarily utilized in research related to cancer immunotherapy and infectious diseases, promoting the activation of innate immunity. Its ability to stimulate TLR7 provides insights into therapeutic strategies aimed at enhancing antitumor immunity and combating viral infections.
  42. TLR7 Agonist

    Guretolimod is a potent Toll-like receptor 7 (TLR7) agonist that activates the immune response through the stimulation of toll-like receptor pathways. It elicits robust antiviral and antitumor activity, making it a valuable tool for research in immunotherapy and infectious disease models. Its role in enhancing antigen presentation and T cell activation positions Guretolimod as an important reagent for studies focused on immune modulation and vaccine development.
  43. TLR7/8 Agonist

    TLR7/8 Agonist 4 TFA is a potent agonist of Toll-like receptor 7 and 8 (TLR7/8), known for its ability to activate innate immune responses. This compound exhibits significant anti-cancer activity, making it a valuable tool for cancer immunotherapy research. It can be utilized in studies exploring TLR-mediated pathways and the development of immune-modulating therapies.
  44. TLR3 Agonist

    Polyinosinic acid is a single-stranded homonucleic acid that functions as an agonist for Toll-like Receptor 3 (TLR3). By activating TLR3 and the associated TRIF pathway, polyinosinic acid enhances cellular immune responses. This reagent is invaluable for research focused on immune regulation and the study of innate immunity mechanisms.
  45. TLR8 Agonist

    TLR8 Agonist 2 Hydrochloride is a highly potent and selective agonist for Toll-like receptor 8 (TLR8), exhibiting an EC50 value of 3 nM in human TLR8 assays. This compound demonstrates significantly lower activity against human TLR7, with an EC50 of 33.33 μM. Due to its specific activation of TLR8, this reagent is valuable for research applications involving immune response modulation and the study of pathogen recognition mechanisms.
  46. TLR8 Agonist

    TLR8 Agonist 2 is a selective activator of Toll-like receptor 8, exhibiting a potent EC50 of 3 nM for human TLR8. This compound demonstrates minimal activity against human TLR7, with an EC50 of 33.33 μM. TLR8 Agonist 2 is valuable for investigating immune responses and therapeutic applications in the modulation of innate immunity.
  47. TLR7/8 Agonist

    TLR7/8 agonist 7 is a novel activator of Toll-like receptors 7 and 8, crucial components in the immune response. This compound stimulates various immune cell types, facilitating immune activation and promoting the synthesis of immune-stimulating antibody conjugate (ISAC) molecules. TLR7/8 agonist 7 is a valuable tool for investigating immune pathways and developing immunotherapeutic strategies.
  48. TLR7 Agonist

    UC-1V150 is a selective agonist of Toll-like receptor 7 (TLR7) that enhances cellular immune responses and exhibits anti-tumor efficacy. This compound is effective in the synthesis of Immune-Stimulating Antibody Conjugates (ISACs), making it a valuable tool for research in immunotherapy and cancer treatment. Its pharmacological properties position UC-1V150 as an important reagent for investigating TLR7-mediated pathways.
  49. TLR-4 Agonist

    3A-MPLA ammonium is a monophosphoryl rri-acyl lipid A that acts as a Toll-like receptor 4 (TLR-4) agonist. It is known to stimulate immune responses by activating the TLR-4 pathway, leading to the production of pro-inflammatory cytokines. This compound is valuable in research applications focused on immunology, vaccine development, and the study of host-pathogen interactions.
  50. TLR4/NF-kB/MAPK Inhibitor

    TLR4/NF-κB/MAPK-IN-1 is an inhibitor targeting the TLR4/NF-κB/MAPK signaling pathways. It exhibits significant anti-neuroinflammatory activity by suppressing the activation of these pathways, leading to reduced inflammatory responses. This compound is particularly useful for research applications focusing on neuroinflammation and related neurodegenerative diseases.

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