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Toll-like Receptor (TLR) Agonist
TLR7/8 Agonist 12 is a potent agonist for human Toll-like Receptors 7 and 8, exhibiting EC50 values of 11 nM and 150 nM, respectively. This compound is capable of immunomodulation, making it a valuable tool for researchers studying innate immune responses and developing therapeutic strategies for various diseases. Its ability to activate these receptors enhances the understanding of TLR-mediated signaling pathways in both basic and applied biomedical research. -
TLR8 Agonist
TLR8 Agonist 7 is a potent agonist of Toll-like receptor 8 (TLR8) with an EC50 of less than 250 nM. It effectively stimulates the secretion of pro-inflammatory cytokine TNFα, exhibiting an EC50 of less than 1 μM. Additionally, TLR8 Agonist 7 demonstrates significant antitumor activity in an MC38-HER2 xenograft mouse model, achieving a tumor growth inhibition rate of 98%. This compound is valuable for research applications focusing on immune response modulation and cancer therapeutics. -
TLR4/CD14 Blocker
IAXO-101 iodide is a specific blocker of TLR4/CD14 signaling. This compound effectively inhibits the innate immune pathway mediated by CD14, demonstrating key biological activities such as enhancing intracortical microelectrode recording capabilities in murine models. Additionally, IAXO-101 iodide has been shown to partially alleviate fetal growth restriction and placental vascular damage, while reducing levels of the inflammatory cytokine TNF-α in pregnant mice with malaria infections. It serves as a valuable research tool for studying gestational malaria and other inflammatory disorders. -
TLR8 Activator
ORN 02 is a synthetic single-stranded U-rich RNA that acts as a Toll-like receptor 8 (TLR8) activator. This reagent consists of six repeats of the UUAU sequence motif, which enhances its ability to stimulate TLR8 signaling. ORN 02 is useful in research applications focused on immune response modulation and the study of RNA-based therapeutics. Its role in TLR8 activation positions it as an important tool for investigating innate immunity and potential therapeutic strategies. -
TLR-4 Agonist
α-Galactosyl FP20 sodium acts as a TLR-4 agonist, playing a significant role in enhancing immune responses. Its primary function as a vaccine adjuvant aids in the potentiation of specific immune reactions, making it valuable for research applications in immunology and vaccine development. This compound supports studies aimed at understanding innate immunity and may inform the design of more effective vaccines. -
TLR4 Agonist
FP-20 sodium is a selective agonist of Toll-like receptor 4 (TLR4) that serves as a potent vaccine adjuvant. It activates the MAPK pathway and promotes NLRP3-dependent inflammasome activation, enhancing immune responses. In mouse vaccination studies using ovalbumin (OVA) antigen, FP-20 sodium demonstrated no toxicity while effectively inducing IgG production, making it a valuable tool for immunological research. -
TLR2 Inducer
SjDX5-53 is a selective TLR2 inducer derived from a 3 kDa peptide sourced from Schistosoma japonicum eggs. This compound effectively inhibits inflammatory Th1 and Th17 responses by inducing tolerogenic dendritic cells (tolDCs) while promoting the generation of regulatory T cells (Tregs) and enhancing their suppressive capacity. SjDX5-53 is primarily employed in research focused on autoimmune and inflammatory diseases, including colitis and psoriasis. -
TLR8 Agonist
TLR8 Agonist 6 is a potent TLR8 agonist, exhibiting an EC50 of 0.052 μM. This compound effectively induces IL-12p40 production in human peripheral blood mononuclear cells (PBMC) with an EC50 of 0.031 μM. TLR8 Agonist 6 is suitable for research applications focused on virus and infection resistance, autoimmunity, and tumor immunology. -
TLR-2/TLR-6 Agonist
Macrophage-activating lipopeptide 2 (MALP-2) is an agonist of Toll-like receptors TLR-2 and TLR-6, which plays a critical role in immune response modulation. MALP-2 enhances phosphorylation of endothelial nitric oxide synthase (eNOS) and stimulates nitric oxide (NO) release from endothelial cells, promoting vasodilation. Additionally, it facilitates the adhesion of white blood cells in endothelium and supports perfusion recovery and collateral vessel growth in hypercholesterolemic Apoe-deficient mouse models during femoral artery ligation experiments. This makes MALP-2 a valuable tool for studying vascular biology and immune response in cardiovascular research. -
TLR8 Agonist
TLR8 Agonist 8 (Compound II-72) acts as a potent agonist for Toll-like receptor 8 (TLR8), exhibiting an effective concentration (EC50) ranging from 0.25 to 1 μM. This compound is stable in both human and murine plasma and stimulates the secretion of cytokine TNFα, with an EC50 of less than 1 μM. Additionally, TLR8 Agonist 8 demonstrates significant antitumor activity, achieving a tumor growth inhibition (TGI) rate of 89% in the MC38-HER2 xenograft mouse model, highlighting its potential for therapeutic applications in oncology and immunotherapy. -
TLR4 Agonist
3D-Monophosphoryl Lipid (14) triethylamine acts as a TLR4 agonist, stimulating Toll-like receptor 4 to initiate immune responses. This compound is utilized as a vaccine adjuvant, enhancing the immunogenicity of vaccines, making it a valuable tool in immunological research and vaccine development. Its ability to modulate immune responses makes it particularly relevant for studies focused on infectious diseases and therapeutic vaccines. -
TLR7 Agonist
TLR7 Agonist 32 is a selective agonist for Toll-like receptor 7 (TLR7), designed for use as a payload in the synthesis of antibody-drug conjugates (ADCs). This compound activates the TLR7 pathway, leading to enhanced immune responses, which may be beneficial in cancer immunotherapy and other therapeutic applications. Research focused on ADC development and related immunological studies can leverage TLR7 Agonist 32 for potential therapeutic advancements. -
TLR4 Agonist
TLR4 Agonist-1 (TEA) is a potent agonist of Toll-like Receptor 4 (TLR4), known for its ability to activate immune responses. This compound effectively induces the production of MIP-1β in RAW 264.7 and MM6 cell lines, making it a valuable tool for studying inflammatory pathways. Its role in modulating TLR4 activity lends itself to research applications in immunology and therapeutic development for inflammatory diseases. -
TLR7/8A Agonist Adjuvant
PVP-037 is a potent agonist for Toll-like receptors 7 and 8 (TLR7/8), functioning as an effective adjuvant in immunological research. This compound elicits robust innate immune activation, significantly enhancing the immune responses to vaccines. PVP-037 is valuable for studies focused on vaccine development and immunotherapy applications. -
TLR4 Ligands
CRX 527 is a ligand of Toll-like receptor 4 (TLR4) that functions as an adjuvant for peptide-based cancer vaccines, demonstrating the ability to enhance anti-tumor immune responses. In addition to its immune-modulating properties, CRX 527 induces hematopoietic stem cell (HSC) differentiation, increases the number of Lin⁻Sca-1⁺c-Kit⁺ (LSK) cells, and promotes their differentiation into macrophages. This reagent activates immune defense mechanisms and provides protective effects on intestinal epithelium against radiation damage, making it valuable for cancer immunotherapy and research in regenerative medicine. -
TLR antagonists
Bazlitoran sodium is an oligonucleotide that serves as an antagonist of Toll-like receptors TLR7, TLR8, and TLR9. It exhibits potential immunomodulatory effects by inhibiting the activation of these receptors, which play crucial roles in the innate immune response. This compound has applications in research focusing on autoimmune disorders, viral infections, and related inflammatory conditions. -
TLR antagonists
CpG-ODN c41 is an oligonucleotide that acts as an antagonist of Toll-like receptor 9 (TLR9). This compound has been shown to modulate immune responses by inhibiting TLR9 activation, making it useful for studies in immunology, inflammation, and autoimmunity. Its application includes the investigation of TLR9-mediated signaling pathways and the development of therapeutic strategies targeting overactive immune responses. -
Toll-like Receptor (TLR) Inhibitor
Tilsotolimod sodium is a synthetic agonist of Toll-like receptor 9 (TLR9), primarily involved in modulating immune responses. It has exhibited significant antitumor activity in preclinical models, making it a valuable reagent for cancer research. Tilsotolimod’s ability to enhance immune system engagement with tumor cells is particularly relevant for studies focused on immunotherapy and tumor immunology. -
TLR1/2 Agonist
Pam3CSK4-Biotin is a biotinylated agonist specifically targeting Toll-like receptors 1 and 2 (TLR1/2). It effectively stimulates immune responses, making it a valuable tool for research in immunology and inflammation. This reagent is commonly utilized in studies assessing TLR signaling pathways and immune system modulation. -
TLR agonist
Sitmutolimod is a CpG oligonucleotide that acts as a Toll-like receptor (TLR) agonist, exhibiting notable antineoplastic activity. By stimulating the immune response through TLR pathways, it enhances the antitumor effects in various cancer models. This compound is primarily utilized in cancer research to investigate immune modulation and the potential for developing novel immunotherapeutic strategies. -
TLR7 Agonist
TLR7 Agonist 5 is a selective TLR7 agonist with an EC50 of approximately 4 nM, facilitating the activation of the Toll-like receptor 7 pathway. This compound is instrumental in studying innate immune responses and has potential applications in cancer immunotherapy and viral infections research. Its ability to enhance cytokine production makes it a valuable tool for investigating TLR7-mediated immune mechanisms. -
TLR4 Receptor Agonist
Defoslimod is a potent TLR4 receptor agonist that functions as an immunomodulator. It activates macrophages and dendritic cells, leading to the secretion of pro-inflammatory cytokines. Additionally, Defoslimod demonstrates significant antitumor activity in preclinical models, making it a valuable tool for research in immunology and cancer therapy. -
TLR-4 Agonist
FP-18 disodium is a TLR-4 agonist that functions as a potent vaccine adjuvant. Its primary mechanism involves the activation of Toll-like receptor 4, which plays a crucial role in enhancing immune responses. This compound is valuable in research aimed at developing vaccines and studying innate immunity pathways. -
TLR7 Antagonist
TLR7 antagonist-1 is a selective antagonist of Toll-like receptor 7 (TLR7), exhibiting an IC50 value of 0.3 nM. It binds specifically to TLR7, inhibiting its activation and subsequently downregulating the c-Rel signaling pathway. This compound effectively reduces the mRNA levels of pro-inflammatory cytokines, such as IL-1β, IL-6, and TNF-α. TLR7 antagonist-1 is particularly relevant for research focused on psoriasis, demonstrating efficacy in alleviating Imiquimod-induced psoriasis-like skin lesions. -
Toll-like Receptor (TLR) Ligand
Ste2Cys is a diacylglycerol cysteine-type lipid molecule that serves as a ligand for Toll-like Receptor 2 (TLR2). It activates the NF-κB signaling pathway, leading to the upregulation of MHC II class molecules on the surface of mouse bone marrow-derived dendritic cells. This compound is valuable for research into the development of immunologic vaccines and enhancing immune responses. -
TLR9 Agonist
ODN M326 is a potent TLR9 agonist that activates the Toll-like receptor 9 pathway, leading to the stimulation of immune responses. It effectively induces the production of pro-inflammatory cytokines such as TNF, making it valuable for enhancing immune activity. ODN M326 is commonly employed as a vaccine adjuvant, promoting stronger and more effective vaccine responses in various research applications. -
TLR8 Agonist
TLR8 Agonist 9 (Compound II-77) is a selective agonist for Toll-like receptor 8 (TLR8), demonstrating an EC50 range of 0.25-1 μM. This compound effectively induces the secretion of the pro-inflammatory cytokine TNFα, with an EC50 of less than 1 μM. Additionally, TLR8 Agonist 9 exhibits significant antitumor activity in the MC38-HER2 xenograft mouse model, achieving a tumor growth inhibition (TGI) rate of 97%, making it a valuable tool for immunotherapy research and cancer studies. -
TLR Agonist
AXC-879 is a Toll-like receptor (TLR) agonist with an EC50 of 157.2 nM. This compound exhibits significant immunostimulatory activity, promoting innate immune responses. Additionally, AXC-879 serves as an antibody-drug conjugate (ADC) cytotoxin and is suitable for ADC synthesis, enabling targeted delivery of therapeutic agents in research applications. -
Stx2a/TLR4 Interaction Inhibitor
NAB815 is a selective inhibitor of the Stx2a/TLR4 interaction, exhibiting a Kd of 0.01 μM. It effectively inhibits neutrophil/Stx2a interactions with an IC50 of 0.057 μg/mL and decreases the formation of Stx2-containing extracellular vesicles from leukocytes and platelets, mitigating their toxic effects in both cellular and animal models. Additionally, NAB815 significantly reduces bacterial loads in the kidneys, urine, and bladders of Escherichia coli-infected mice, making it a valuable tool for investigating hemolytic uremic syndrome (HUS). -
TLR9 Inhibitor
TLR9-IN-2 is a selective inhibitor of Toll-like receptor 9 (TLR9), with an IC50 of 25 nM, demonstrating significant selectivity over TLR7 and TLR8 (1400 nM and > 50,000 nM, respectively). This compound is valuable for investigating the role of TLR9 in various biological contexts, particularly in studies related to fibrosis, autoimmune conditions, and inflammatory diseases. Its specificity makes it an important tool for elucidating TLR9-mediated signaling pathways and potential therapeutic interventions. -
TLR2 Agonist
TLR2 Agonist 1 is a highly potent agonist for human toll-like receptor 2 (TLR2), exhibiting an EC50 of 116 pM. It activates NF-κB promoter activity through TLR2/TLR1 heterodimerization, making it a valuable tool for studying TLR-mediated immune responses. This compound is applicable in research focused on inflammation, innate immunity, and potential therapeutic strategies involving TLR pathways. -
TLR7/8 Agonist
3M-011 is a potent dual agonist of toll-like receptors TLR7 and TLR8, functioning primarily as a cytokine inducer. It has demonstrated significant efficacy in inhibiting H3N2 influenza viral replication in the nasal cavity. Additionally, 3M-011 serves as an effective adjuvant to radiotherapy, promoting both local and systemic immune responses that enhance antitumor activity. Research applications include immunotherapy, virology, and enhancing the efficacy of cancer treatments. -
TLR-4 Agonist
α-Rhamnosyl FP20 sodium acts as an agonist for Toll-like receptor 4 (TLR-4), playing a crucial role in immune activation. This compound is primarily utilized as a vaccine adjuvant, enhancing the efficacy of vaccine responses by stimulating the innate immune system. Its application in research includes the development and optimization of vaccine formulations aimed at improving immunogenicity. -
TLR4 Agonist
FP20Rha is a potent agonist of Toll-like receptor 4 (TLR4). It is designed to enhance immune responses and significantly improve vaccine efficacy against Pseudomonas aeruginosa. This compound is valuable for research applications focusing on vaccine development and infectious disease models. -
TLR7 Agonist
TLR7 Agonist 23 is a potent Toll-Like Receptor 7 (TLR7) agonist with an EC50 of 0.15 µM. This compound activates TLR7, triggering immune responses, making it a valuable tool for studying immunological diseases and exploring potential therapeutic applications in immune modulation. -
Toll-like Receptor (TLR)
Chitohexaose hexahydrochloride is a chitosan oligosaccharide targeting Toll-like Receptor 4 (TLR4). It exhibits anti-inflammatory properties by binding to the active sites of TLR4, leading to the inhibition of lipopolysaccharide (LPS)-induced inflammation. This compound is valuable for research applications focused on immune response modulation and the study of inflammatory pathways. -
TLR4 Ligand
TLR4-IN-1 is a selective TLR4 ligand inhibitor that effectively diminishes cell viability in RAW264.7 macrophages with an IC50 of 1.02 μM. This compound significantly reduces the release of pro-inflammatory cytokines, including TNF-α, IL-1β, and IL-6, demonstrating potent anti-inflammatory effects in models of rheumatoid arthritis in rats. Its targeted mechanism makes TLR4-IN-1 a valuable tool for studying the role of TLR4 in inflammatory processes and related therapeutic applications. -
TLR7 Agonist
TLR7 Agonist 16 is a potent agonist targeting Toll-like receptor 7 (TLR7) with an EC50 of 18 nM. It effectively stimulates the activation of mouse macrophages and human peripheral blood mononuclear cells (hPBMCs) at low-nanomolar concentrations. This compound is valuable for research applications involving immune response modulation and the study of TLR7-associated pathways. -
TLR7/8 Agonist
m-AM-BBIQ is a dual agonist for Toll-like receptors 7 and 8 (TLR7/8), exhibiting EC50 values of 0.12 μM and 1.7 μM for human TLR7 and TLR8, respectively. This compound elicits strong immune responses, making it a valuable tool in immunology research and vaccine development. Its ability to activate TLR7/8 pathways can facilitate studies on innate immune activation and the potential enhancement of antiviral responses. -
TLR7/8 Agonist
Gardiquimod hydrochloride is a potent TLR7/8 agonist that activates the immune response. It has been shown to inhibit HIV-1 infection in macrophages and effectively activates peripheral blood mononuclear cells (PBMCs). This compound selectively stimulates TLR7 at concentrations below 10 μM, making it a valuable tool for research in immunology and antiviral therapy. -
TLR7 Agonist
TLR7 Agonist 8 (compound IIb-34) selectively activates Toll-like receptor 7 (TLR7) with an EC50 of approximately 4 nM. This potent agonist stimulates immune responses and plays a critical role in enhancing antiviral and antitumor immunity. It is valuable for research applications related to immunology and the development of therapeutics targeting TLR7 pathways. -
TLR7 Agonist
TLR7 Agonist 15 is a potent TLR7 activator that exhibits an EC50 of 18 nM. This compound effectively stimulates the activation of mouse macrophages and human peripheral blood mononuclear cells (hPBMCs) at low nanomolar concentrations. It holds potential applications in immunology research, particularly in studies focused on innate immune responses and antiviral mechanisms. -
Toll-like Receptor (TLR) Inhibitor
Tilsotolimod is a synthetic agonist of Toll-like receptor 9 (TLR9) involved in modulating immune responses. It has exhibited significant antitumor activity in preclinical models, making it a valuable reagent for cancer immunotherapy research. This compound is utilized in studies focused on enhancing the immune system's ability to target and eradicate tumors. -
TLR-9 Agonist
Cobitolimod sodium is a TLR-9 agonist that exhibits anti-inflammatory properties through its action on immune signaling pathways. This DNA oligonucleotide effectively inhibits Th17 cell activation while enhancing the expression of the anti-inflammatory markers FoxP3 and IL-10. By targeting and inhibiting the IL-17 signaling pathway, Cobitolimod sodium is valuable for research focused on inflammatory diseases and immune modulation. -
TLR4 Activator
CCL-34 is a potent Toll-like receptor 4 (TLR4) activator that effectively promotes dendritic cell maturation by significantly increasing CD83 expression and IL-12p70 production in a dose-dependent manner. This compound enhances the allostimulatory capacity of dendritic cells, leading to increased proliferation and IFN-γ secretion in naive CD4+CD45+RA+ T cells. Additionally, CCL-34 has demonstrated its capacity to boost antigen presentation in murine models with doxorubicin-treated colorectal cancer cells, making it valuable for research into immune stimulation and therapeutic strategies. -
TLR7/8 Agonist
TLR7/8 Agonist 9 is a potent agonist of Toll-like receptors 7 and 8, exhibiting EC50 values of 40 nM and 23 nM, respectively, for human TLR7 and TLR8. This compound demonstrates anti-tumor activity and enhances the efficacy of PD-1/PD-L1 blockade, making it a valuable tool for cancer immunotherapy research. It is suitable for studies investigating immune modulation and therapeutic strategies in oncological applications. -
TLR7 Agonist
TLR7 Agonist 33 is a potent activator of Toll-like receptor 7 (TLR7) with an EC50 of 1 nM. This compound exhibits significant immunostimulatory activity, making it suitable for cancer research and therapeutic applications targeting TLR signaling pathways. Its ability to enhance innate immune responses positions TLR7 Agonist 33 as a valuable tool in studying the role of TLR7 in tumor immunity and potential cancer treatments. -
TLR7/8 Antagonist
TLR7/8 Antagonist 1 is a potent antagonist of Toll-like receptors 7 and 8, exhibiting IC50 values of 3.91 μM and 2.19 μM, respectively. This imidazoquinoline derivative is instrumental in modulating immune responses and serves as a valuable tool in research applications targeting infectious diseases, cancer, and autoimmune disorders. Its unique mechanism of action enables the exploration of TLR-mediated pathways, contributing to the development of novel immunomodulatory therapies. -
TLR-9 Agonist
Cobitolimod is a TLR-9 agonist that exhibits anti-inflammatory activity through the modulation of immune responses. It effectively suppresses Th17 cell activity while promoting the expression of anti-inflammatory markers such as FoxP3 and IL-10. This action inhibits the IL-17 signaling pathway, making Cobitolimod valuable for research investigating inflammatory diseases and immune regulation mechanisms. -
TLR7 Agonist
TLR7 Agonist 26 is a potent agonist of Toll-like receptor 7 (TLR7), exhibiting an EC50 value of 225.5 nM. This compound demonstrates significant immunopotentiating effects, making it a valuable tool in immunological research. It is suitable for studies focused on enhancing immune responses and investigating TLR7-mediated pathways in various biological contexts.

