Catalog No.
Product Name
Application
Product Information
Citations
-
TLR Antagonist
ODN TTAGGG is a TLR9, AIM2, and cGAS antagonist that functions as an inhibitory oligonucleotide. This compound inhibits the activation of the AIM2 inflammasome as well as cGAS by competing with endogenous DNA. As a result, ODN TTAGGG obstructs AIM2-mediated pyroptosis and reduces IL-18 production. Its immunosuppressive properties make it useful in research related to autoimmune diseases, including lupus erythematosus. -
TLR7/TLR9 Inhibitor
AT791 is a potent inhibitor of Toll-like receptors 7 and 9 (TLR7/TLR9), demonstrating strong oral bioavailability. This compound effectively blocks TLR7 and TLR9 signaling pathways in a range of human and murine cell types, as well as inhibiting DNA-TLR9 interactions in vitro. AT791 is applicable in research focused on immune modulation and the characterization of TLR-mediated signaling. -
TLR3/7/9 Inhibitor
ODN 2088 is a potent inhibitor of Toll-like receptors 3, 7, and 9 (TLR3, TLR7, TLR9), demonstrating a strong capacity to modulate immune responses. This compound effectively suppresses the release of key pro-inflammatory cytokines, including interferon-alpha (IFN-α) and interleukin-6 (IL-6), without exhibiting cytotoxic effects. ODN 2088 is valuable for research applications focused on understanding TLR-mediated signaling pathways and their roles in various immune-related conditions. -
TLR2/TLR4 Antagonist
Sparstolonin B is a selective antagonist of Toll-like receptors 2 and 4 (TLR2/TLR4), effectively inhibiting TLR2- and TLR4-mediated inflammatory signaling pathways. This compound demonstrates notable anti-HIV and anticancer properties, making it valuable for research into immune modulation and cancer therapy. Its ability to block key inflammatory responses adds significance to its use in studying various diseases linked to TLR signaling. -
TLR9 Agonist
ODN 2395 is a C class oligodeoxynucleotide that functions as a TLR9 agonist, promoting immune responses. Its primary application is as a vaccine adjuvant, enhancing the efficacy of immunological vaccines. This compound facilitates the activation of dendritic cells and B cells, thereby driving robust adaptive immunity. Sequence: 5'-tcgtcgttttcggcgc:gcgccg-3'. -
TLR9 Agonist
ODN 1018 is a Toll-like receptor 9 (TLR9) agonist functioning as an immune modulator. It demonstrates adjuvant activity by enhancing CD8+ T cell responses when combined with liposomal nanoparticles encapsulating ovalbumin (OVA) peptides. Additionally, ODN 1018 effectively induces prolonged suppression of allergic airway inflammation, making it a valuable tool for research into allergic asthma and systemic lupus erythematosus. -
Toll-like Receptor (TLR) Inhibitor
Okanin is a potent Toll-like Receptor (TLR) inhibitor derived from the flowering plant Coreopsis tinctoria. It exhibits significant biological activity by attenuating lipopolysaccharide (LPS)-induced microglial activation via the inhibition of the TLR4/NF-κB signaling pathway. This compound is useful for research applications focusing on neuroinflammation and the modulation of immune responses in microglial cells. -
TLR7/8 Inhibitor
Enpatoran hydrochloride is a dual inhibitor of Toll-like receptors 7 and 8, demonstrating potent activity with IC50 values of 11.1 nM and 24.1 nM, respectively, in HEK293 cells. This compound is selectively inactive against TLR3, TLR4, and TLR9, effectively blocking both synthetic and natural RNA ligands. Enpatoran hydrochloride exhibits favorable pharmacokinetic profile in vivo, making it a valuable tool for research into innate and adaptive autoimmunity pathways. -
TLR7/8 Agonist
CL097 is a potent agonist of Toll-like receptors 7 and 8 (TLR7/8), eliciting a robust pro-inflammatory cytokine response in macrophages. By priming NADPH oxidase, CL097 enhances fMLF-stimulated reactive oxygen species (ROS) production. This compound is valuable for research applications in immunology and inflammation studies, particularly in understanding innate immune responses. -
TLR9 Inhibitor
TLR9-IN-1 is a potent and selective inhibitor of Toll-like receptor 9 (TLR9), exhibiting an IC50 value of 7 nM for human TLR9. This compound is valuable for studying diseases linked to aberrant immune responses, making it an important tool in immunological research and therapeutic development. Researchers can utilize TLR9-IN-1 to explore the modulation of TLR9 pathways in various inflammatory and autoimmune conditions. -
TLR8 Agonist
Selgantolimod is a potent and selective agonist of toll-like receptor 8 (TLR8). This orally active compound has demonstrated significant biological activity in activating the immune response, making it a valuable agent in the treatment of hepatitis B virus (HBV) and human immunodeficiency virus (HIV) infections. Its mechanism of action supports research into immunotherapeutic strategies targeting viral pathogens. -
TLR7/8 Agonist
Gardiquimod is an imidazoline compound that acts as an agonist for Toll-like receptors 7 and 8 (TLR7/8). This reagent has been shown to inhibit HIV-1 infection in macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 at concentrations below 10 μM, making it a valuable tool in immunological research and studies related to viral infections. -
TLR8 Agonist
TL8-506 is a selective TLR8 agonist with an EC50 of 30 nM. This compound exhibits immunomodulatory properties, making it a valuable tool for investigating therapeutic approaches in tuberculosis and cancer immunotherapy. Researchers can leverage TL8-506 to enhance immune responses and study the underlying mechanisms of TLR8-mediated signaling. -
TLR-9 Agonist
ODN 1668 is a TLR-9 agonist classified as a class B CpG oligodeoxynucleotide (ODN). This reagent exhibits significant immune regulatory properties, enhancing IgG2 antibody levels and promoting T cell and B cell immune responses, making it useful in vaccine adjuvant research. Additionally, ODN 1668 induces an antimicrobial immune response through a CaTLR9-dependent pathway in groupers. Sequence: 5'-tccatgacgttcctgatgct-3’. -
Toll-like Receptor (TLR) Agonist
TLR7/8 Agonist 1 is a dual agonist of Toll-like Receptors 7 and 8, belonging to the imidazoquinoline class. This compound activates the innate immune response by engaging TLR7 and TLR8, leading to the production of pro-inflammatory cytokines. It has significant applications in immunological research, particularly in studies related to viral infections, cancer immunotherapy, and the modulation of immune responses. -
TLR7/TLR8 Inhibitor
TLR7/8-IN-1 is a potent inhibitor of Toll-like receptors 7 and 8, which play critical roles in the immune response. This compound exhibits strong potential in modulating inflammatory pathways associated with autoimmune diseases. It serves as a valuable tool for researchers investigating the therapeutic targeting of TLR7 and TLR8 in various immunological studies. -
Toll-like Receptor (TLR) Agonist
Neoseptin 3 is an agonist of Toll-like receptor 4 (TLR4) and myeloid differentiation factor 2 (MD-2), exhibiting an EC50 of 18.5 μM. This compound promotes innate immune responses and enhances cytokine production, making it a valuable tool for studying immune system activation. Neoseptin 3 is suitable for research on inflammatory diseases and immune modulation. -
TLR8 Agonist
CL075 is a selective TLR8 agonist that activates the MyD88-dependent signaling pathway, leading to the production of inflammatory cytokines and type I interferons (IFNs). This compound enhances NF-κB and IRF7 activation, contributing to immune modulation. It is primarily used in research applications focused on inflammation and immune response mechanisms. -
TLR3 Ligand
Polyinosinic acid sodium is the sodium salt of polyinosinic acid, a single-stranded homonucleic acid that serves as a Toll-like Receptor 3 (TLR3) ligand. By activating TLR3, polyinosinic acid sodium enhances the cellular immune response through the TRIF signaling pathway. This reagent shows potential for use in studies focused on immune regulation and adjuvant therapies in various research applications. -
TLR4 Inhibitor/PROTAC Linker
TLR4-IN-C34-C2-COOH is a TLR4 inhibitor that serves as a PROTAC linker. It demonstrates significant potential in the modulation of inflammatory responses, particularly in studies involving acute myocardial injury. By targeting TLR4 in enterocytes and macrophages, TLR4-IN-C34-C2-COOH effectively reduces systemic inflammation in murine models of endotoxemia and necrotizing enterocolitis, making it a valuable tool for research in inflammation-related pathways. -
TLR 7 Agonist
Loxoribine, a guanosine analog, functions as a selective Toll-like receptor (TLR) 7 agonist. This compound exhibits significant anti-viral and anti-tumor activities, making it valuable for research applications in immunotherapy and cancer treatment. Its oral bioavailability expands its potential for in vivo studies. -
TLR7 Agonist
DSR-6434 is a highly potent and selective agonist of Toll-like receptor 7 (TLR7), exhibiting EC50 values of 7.2 nM for human TLR7 and 4.6 nM for mouse TLR7. This compound demonstrates significant antitumor activity, making it a valuable tool for studying cancer immunotherapy and TLR7 signaling pathways in various research applications. -
TLR7 Agonist
CL264 is a selective agonist of Toll-like receptor 7 (TLR7), primarily utilized for examining innate immune signaling pathways. This compound enhances the activation of immune responses through TLR7 stimulation, making it a valuable tool for research in immunology and inflammation. Its application extends to understanding the mechanisms of antiviral responses and potential therapeutic strategies targeting TLR-mediated immune modulation. -
Toll-like Receptor (TLR) Antagonist
TLR7/8/9-IN-1 is a potent small molecule antagonist targeting Toll-like receptors 7, 8, and 9, with an IC50 value of 43 nM. This compound effectively inhibits TLR-mediated signaling pathways, playing a crucial role in the immune response. It is valuable for research applications focused on inflammatory diseases, autoimmune disorders, and the modulation of innate immunity. -
TLR9 Agonist
CpG ODN 10101 is a TLR9 agonist, designed as a synthetic oligodeoxynucleotide modified with phosphate thioester. This compound activates B cells and plasmacytoid dendritic cells, leading to enhanced production of cytokines and chemokines, including interferon-α and IP-10. By modulating innate immunity and promoting Th1 adaptive responses, CpG ODN 10101 demonstrates antiviral properties and enhances vaccine immunogenicity, highlighting its potential as an immunomodulator and vaccine adjuvant in the development of therapies for chronic hepatitis C and various infectious diseases. -
TLR4 Antagonist
CAY10614 is a potent TLR4 antagonist that inhibits lipid A-induced activation of the TLR4 receptor, exhibiting an IC50 of 1.675 μM. This compound has demonstrated the ability to improve survival rates in mouse models of lethal endotoxin shock. CAY10614 is valuable for research applications investigating TLR4-mediated inflammatory responses and the development of therapeutic strategies targeting sepsis and other endotoxin-related conditions. -
TLR9 Antagonist
CPG-52364 is a TLR9 antagonist that exhibits inhibitory activity against TLR9 in the HEK293-hTLR9 cell line, with an IC50 value of 4.6 nM. This compound is valuable for research applications investigating immune response modulation, particularly in studies related to autoimmune diseases and inflammation. Its specificity for TLR9 makes it a useful tool for exploring the therapeutic potential of TLR modulation in various biological contexts. -
TLR7/8 Agonist
CL097 hydrochloride is a potent agonist of Toll-like receptors 7 and 8 (TLR7/8) that activates pro-inflammatory cytokine production in macrophages. This compound also facilitates NADPH oxidase priming, leading to enhanced reactive oxygen species (ROS) generation upon fMLF stimulation. CL097 is valuable in research applications related to immune response and inflammation. -
TLR4 inhibitor
TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis. -
TLR-3 Agonist
Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic analog of double-stranded RNA that serves as an agonist for toll-like receptor 3 (TLR3) and RIG-I-like receptors, including RIG-I and MDA5. This compound enhances both innate and adaptive immune responses, making it valuable in vaccine development as an adjuvant. Additionally, Poly(I:C) influences the tumor microenvironment and can directly induce apoptosis in cancer cells, highlighting its potential applications in cancer immunotherapy and research. -
PROTAC CSK Degrader
DB-3-291 is a potent and selective PROTAC degrader targeting the protein CSK, exhibiting a Kd of 1 nM. This compound facilitates the degradation of CSK through its specific interaction with the E3 ligase, enabling in-depth studies of CSK-related biological pathways and providing insights into potential therapeutic strategies. It is valuable for researchers investigating targeted protein degradation and cancer biology. -
TLR4 Agonist
GlcNAc-MurNAc is a disaccharide that acts as a TLR4 agonist, exhibiting a binding affinity (Kd) of 383 μM for murine TLR4. This compound directly interacts with TLR4, subsequently activating the downstream NF-κB and IRF signaling pathways. Research indicates that GlcNAc-MurNAc ameliorates dextran sulfate sodium salt (DSS)-induced colitis in mice via a TLR4-dependent mechanism, making it a valuable tool for the investigation of inflammatory bowel disease. -
TLR3 Agonist
Polyinosinic-polycytidylic acid sodium is a synthetic analogue of double-stranded RNA and acts as an agonist for toll-like receptor 3 (TLR3) and RIG-I-like receptors. It serves as a potent immunomodulator, enhancing both innate and adaptive immune responses, making it valuable for vaccine development. Additionally, Poly(I:C) sodium can influence the tumor microenvironment and directly induce apoptosis in cancer cells, thus providing significant potential in cancer research and therapy. -
TLR9 Agonist
ODN 1826 is a class B CpG oligodeoxynucleotide that acts as an agonist for Toll-like receptor 9 (TLR9). It stimulates the production of nitric oxide (NO) and inducible nitric oxide synthase (iNOS), promoting apoptosis and enhancing immune surveillance. This compound is also associated with increased aortic atherosclerotic plaque size and exhibits antitumor activity against various cancer types, including lung cancer, glioma, and melanoma. ODN 1826 is valuable for researching immune response mechanisms and potential cancer therapies. -
TLR7/8 Antagonist
Afimetoran is a selective and highly bioavailable antagonist of Toll-like receptors 7 and 8 (TLR7/8). It effectively inhibits TLR7/8-mediated activation of the NF-κB signaling pathway and can reverse TLR7-induced resistance to steroid-driven apoptosis in plasmacytoid dendritic cells. This compound is particularly relevant for research into inflammation and autoimmune diseases, including systemic lupus erythematosus. -
TLR9 Agonist
Agatolimod is a Toll-like receptor 9 (TLR9) agonist and immunomodulator with an EC50 of 180 nM. It activates TLR9 and upregulates TLR6 expression, initiating downstream signaling through IRAK4, IRF5, and IRF7. Agatolimod enhances Th1-type immune responses and promotes the activation of various immune cells, leading to increased antigen presentation, antibody regulation, cytokine secretion, apoptosis, and enhanced cytotoxicity. This compound is relevant for research into COVID-19, breast cancer, lung adenocarcinoma, HPV-related tumors, melanoma, and salmonellosis. -
TLR2/4 Inhibitor
Robinin is a flavonoid that acts as an inhibitor of Toll-like receptors 2 and 4 (TLR2/4), modulating the TGF-β, TLR4/NF-κB, and TLR2-PI3k-AKT signaling pathways. This compound demonstrates significant anti-inflammatory and anti-tumor properties. Additionally, Robinin has been shown to enhance the anti-inflammatory effects of Methotrexate in experimental arthritis models and may mitigate cardiac toxicity induced by Doxorubicin. These attributes make Robinin a valuable reagent for research applications in inflammation and cancer therapy. -
COX-2/MMP-7/TLR4 Inhibitor
Isofraxidin is a coumarin compound derived from *Acanthopanax senticosus* that exhibits anti-invasive and anti-inflammatory properties. It inhibits MMP-7 expression and suppresses cell invasion in human hepatoma cells by reducing ERK1/2 phosphorylation. Isofraxidin also downregulates the expression of iNOS and COX-2 and inhibits the formation of the TLR4/myeloid differentiation protein-2 (MD-2) complex. -
TLR1/2 agonist
CU-T12-9 is a specific and potent agonist of the Toll-like receptor 1/2 (TLR1/2) heterodimer, with an EC₅₀ of 52.9 nM in the HEK-Blue hTLR2 SEAP assay. It selectively activates TLR1/2 without affecting TLR2/6 and stimulates both innate and adaptive immune responses. CU-T12-9 signals through the NF-κB pathway, leading to elevated expression of downstream effectors such as TNF-α, IL-10, and iNOS, making it a valuable tool for immunological and inflammatory research. -
TLR7 Agonist
SMU-L11-R is a selective TLR7 agonist that demonstrates an EC50 of 0.012 μM for human TLR7. This compound specifically activates TLR7, recruits MyD88, and initiates the MAPK/NF-κB signaling pathways, resulting in the secretion of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6 in both mouse and human peripheral blood mononuclear cells. Additionally, SMU-L11-R promotes M1-like macrophage polarization and exhibits synergistic anti-tumor effects in combination with PD-L1 inhibitors through the upregulation of CD8+ T cells, making it a valuable tool for research in colorectal cancer. -
TLR2 Agonist
Pam2CSK4 is a TLR2 agonist that activates immune signaling pathways, leading to the expression of inducible nitric oxide synthase (iNOS) and nitric oxide (NO) in macrophage cell lines through TBK1 and MyD88. This compound stimulates the NF-κB and Bruton's tyrosine kinase pathways in platelets, enhancing interactions between platelets and endothelial cells. Pam2CSK4 promotes the expansion of myeloid-derived suppressor cells (MDSCs) and can suppress anti-tumor immune responses in the tumor microenvironment. Its applications span various diseases, including thromboinflammatory conditions, sepsis, atherosclerosis, and certain cancers, making it a valuable tool in immunological and therapeutic research. -
PI3K/Akt/mTOR signaling pathway Inhibitor, TLR4 signaling Inhibitor
25(R,S)-Ruscogenin is a potent inhibitor of the PI3K/Akt/mTOR and TLR4 signaling pathways. This compound effectively suppresses hepatocellular carcinoma (HCC) metastasis by decreasing the expression of matrix metalloproteinases (MMP-2 and MMP-9), uPA, VEGF, and HIF-1α. Additionally, 25(R,S)-Ruscogenin mitigates LPS-induced apoptosis in pulmonary endothelial cells, highlighting its potential for applications in cancer research and inflammatory disease studies. -
Selective Intranasal TLR7 Agonist
GSK2245035 maleate is a selective intranasal agonist of Toll-Like receptor 7 (TLR7), exhibiting potent Type-1 interferon (IFN) stimulating activity with pEC50 values of 9.3 for IFNα and 6.5 for TNFα. This compound effectively reduces allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 maleate is primarily utilized in research focused on asthma and other Th2-mediated allergic responses. -
TLR Inhibitor
ETI60 is a selective Toll-like receptor (TLR) inhibitor that primarily targets the nucleoside-binding Site I on TLR7 and TLR9, with IC50 values of 0.68 μM and 0.12 μM, respectively. This compound effectively inhibits endosomal TLR-mediated pro-inflammatory signaling, demonstrating nanomolar activity in cellular, biophysical, and in vivo assays. ETI60 modulates the expression of inflammation-related genes and has shown efficacy in alleviating symptoms in mouse models of psoriasis and systemic lupus erythematosus (SLE). This reagent is valuable for research involving autoimmune and inflammatory diseases. -
TLR Inhibitor
ETI41 is a selective Toll-like receptor (TLR) inhibitor that targets the nucleoside-binding Site I on TLR7 and TLR9, demonstrating IC50 values of 0.63 μM and 0.16 μM, respectively, while sparing surface TLRs. This compound effectively inhibits endosomal TLR-mediated pro-inflammatory signaling, displaying potent nanomolar activity across cellular, biophysical, and in vivo assays. ETI41 suppresses the expression of inflammation-associated genes and improves symptoms in murine models of psoriasis and systemic lupus erythematosus (SLE). It is valuable for research into autoimmune and inflammatory diseases. -
TLR9 Antagonist
TLR9 antagonist 1 is a selective toll-like receptor 9 (TLR9) antagonist that exhibits an IC50 of 0.1 nM for human TLR9, demonstrating a significant preference over TLR2, TLR4, TLR5, TLR7, and TLR8. This compound is known to exacerbate symptoms in systemic lupus erythematosus (SLE) mouse models by increasing levels of anti-dsDNA and anti-Sm antibodies. TLR9 antagonist 1 is valuable for research in inflammatory and autoimmune diseases, particularly in the study of disorders such as lupus and arthritis. -
TLR3/9 Inhibitor
M199 is a selective inhibitor of TLR3 and TLR9 signaling pathways. This compound effectively induces the secretion of pro-inflammatory cytokines, including IL-6, IL-8, and TNFα, in human peripheral blood mononuclear cells (PBMCs). M199 is utilized in research to investigate immune response modulation and the role of TLR signaling in various biological processes. -
Selective Intranasal TLR7 Agonist
GSK2245035 is a selective intranasal agonist for Toll-Like Receptor 7 (TLR7), exhibiting potent Type-1 interferon (IFN) stimulation, with pEC50 values of 9.3 for IFNα and 6.5 for TFNα. This compound demonstrates efficacy in suppressing allergen-induced Th2 cytokine production in human peripheral blood cell cultures, making it a valuable tool for asthma research. Its unique mechanism of action highlights its potential in studying immune responses and therapeutic applications in allergic conditions.
