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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
TLR2/9 Antagonist
TLR2/9 Antagonist 1 is a reversible covalent antagonist targeting Toll-like receptors 2 and 9, with IC₅₀ values of 0.5 μM for TLR2/TLR6, 0.6 μM for TLR2/TLR1, and 0.32 μM for TLR9. This compound selectively inhibits TLR2 and TLR9 without significant effects on other TLR subtypes. TLR2/9 Antagonist 1 is valuable for investigating inflammation-related pathology in central nervous system diseases and malignancies. -
TLR4/NF-κB Inhibitor
Ligusticum cycloprolactam is a potent TLR4/NF-κB inhibitor with significant anti-inflammatory properties. It has been shown to alleviate renal injury by effectively disrupting the TLR4/NF-κB signaling pathway in both in vivo and in vitro models. In studies, Ligusticum cycloprolactam reduces serum uric acid levels, diminishes tubular damage, and decreases inflammatory infiltration and interstitial collagen deposition, leading to improved renal function. This compound serves as a valuable reagent for research into hyperuricemic nephropathy. -
TLR1/2 Agonist
SMU-C409 is a Toll-like receptor 1/2 (TLR1/2) agonist, exhibiting an EC50 of 65 nM in HEK-Blue hTLR2 cells. It activates the TLR1/2–MyD88–NF-κB signaling pathway, leading to increased secretion of pro-inflammatory cytokines TNF-α and IL-1β, which promotes robust immune cell activation. With low toxicity observed in vitro, SMU-C409 serves as a valuable tool for cancer immunotherapy research. -
TLR9 Antagonist
TLR9 Antagonist 2 is a highly selective antagonist that targets Toll-like receptor 9 (TLR9), demonstrating an IC50 of 13 nM against human TLR9. This compound effectively inhibits the CpG-induced production of the pro-inflammatory cytokine IL-6. TLR9 Antagonist 2 is valuable for research into systemic inflammation mediated by TLR9, including studies focused on conditions like sepsis. -
TLR7 Agonist
TLR7 Agonist 31 is a selective agonist of Toll-Like Receptor 7 (TLR7), exhibiting an EC50 of 31 nM. This compound plays a significant role in activating innate immune responses, making it a valuable tool for cancer research studies. Its ability to stimulate TLR7 facilitates the exploration of immune-modulatory pathways in tumor microenvironments. -
TLR7 Agonist
TLR7 Agonist 17 is a potent agonist of Toll-like receptor 7 (TLR7), exhibiting EC50 values of 12 nM for human TLR7 and 17 nM for mouse TLR7. This compound demonstrates significant anticancer activity, making it valuable for research applications targeting immune modulation and cancer immunotherapy. Its ability to activate TLR7 pathways provides insights into potential therapeutic strategies for harnessing the immune system in oncology. -
TLR7 Agonists
TLR7 Agonist 19 is a selective agonist of Toll-like receptor 7 (TLR7), known for its superior pharmacokinetic properties. This compound exhibits significant immunostimulatory activity and demonstrates synergistic antitumor effects, making it valuable for cancer immunotherapy research. Its role in enhancing antiviral responses further supports its potential in studying various immune-related applications. -
TLR Inhibitor
AN-3485 hydrochloride is a benzoxaborole analogue that acts as an antagonist of the Toll-like receptor (TLR) pathway. This compound effectively inhibits TLR-mediated secretion of inflammatory cytokines, demonstrating significant anti-inflammatory properties. Additionally, AN-3485 hydrochloride exhibits potential anti-tumor activity, making it a valuable reagent for research applications focused on inflammation and cancer biology. -
TLR7/8 Agonist
ORN 06 is a TLR7/8 agonist that consists of a U-rich single-stranded RNA with six repeats of the UUG sequence motif. This compound activates TLR7/8 pathways in human systems and TLR7 pathways in murine models, promoting immune responses. ORN 06 is utilized in research focused on immunotherapy and the modulation of innate immune signaling. -
TLR9 agonist
Nelitolimod is a TLR9 agonist that acts as a CpG oligonucleotide. It is known to stimulate immune responses by activating Toll-like receptor 9, leading to enhanced production of pro-inflammatory cytokines. This compound is primarily utilized in immunological research, including studies on innate immunity, cancer immunotherapy, and vaccine development. -
TLR9 agonist
GNKG168 is a synthetic, 21-mer unmethylated CpG oligodeoxynucleotide that serves as a TLR9 agonist. It exhibits potent immunostimulatory activity, promoting the activation of innate and adaptive immune responses. This reagent is valuable for research applications focusing on immune modulation, vaccine development, and the study of autoimmune diseases. -
TLR2/1 Agonist
WYJ-2 is a selective agonist for toll-like receptor 2/1 (TLR2/1), exhibiting an EC50 of 18.57 nM in human TLR2 and TLR1 cotransfected HEK 293T cells. This compound induces pyroptosis, a form of programmed cell death, and demonstrates significant anticancer activity against non-small cell lung cancer (NSCLC). WYJ-2 is valuable for research in immunology and cancer therapy. -
TLR1/2 Heterodimer Agonist
SMU-C68 is a selective small-molecule agonist of the TLR1/2 heterodimer, with an EC50 value of 0.009 μM. It effectively activates the NF-κB and MAPK signaling pathways, leading to the release of pro-inflammatory cytokines such as TNF-α and IL-1β. This compound is a valuable tool for investigating mechanisms of inflammation and cancer biology in research applications. -
TLR7/8 Inhibitor
KBD4466 is a potent inhibitor of Toll-like receptors 7 and 8 (TLR7/8), demonstrating IC50 values of 0.9 nM and 2.8 nM, respectively. This compound effectively reduces the expression of inflammatory cytokines such as IL-6 and IFN-α. KBD4466 has shown promise in improving disease progression and survival in the BXSB/MpJ mouse model of Systemic Lupus Erythematosus (SLE), making it a valuable tool for research in autoimmune diseases. -
TLR antagonists
Bazlitoran is a potent antagonist of Toll-like receptors 7, 8, and 9 (TLR7, TLR8, and TLR9). This oligonucleotide modulates immune responses by inhibiting TLR-mediated signaling pathways, making it an essential tool for studying the role of these receptors in various inflammatory diseases and autoimmune conditions. Research applications include the exploration of therapeutic strategies targeting TLR signaling in infectious diseases and cancer. -
TLR9 agonist
Litenimod is a potent TLR9 agonist that activates both innate and adaptive immune responses. By enhancing the recognition of pathogen-associated molecular patterns, it promotes a robust immune reaction, making it a valuable tool for research into immune modulation, vaccine development, and adjuvant therapies. Litenimod's ability to stimulate TLR9 provides insights into its therapeutic potential in various immunological disorders. -
TLR7 Agonist
TLR7 Agonist 20 is an imidazoquinoline analogue that functions as a potent agonist for the Toll-like receptor 7 (TLR7), exhibiting an EC50 value of 0.23 μM for human TLR7. This compound demonstrates significant adjuvant effects on antibody responses, notably enhancing spike antibody levels and promoting a robust T helper 1 (Th1) immune response characterized by increases in IgG2b, IgG2c, and IgG1 production. TLR7 Agonist 20 is suitable for applications in immunological research and the development of vaccine adjuvants. -
TLR7 Inhibitor
TLR7-IN-1 is a selective inhibitor of Toll-like receptor 7 (TLR7) with an EC50 value of 0.001 µM. This compound effectively modulates TLR7 signaling pathways, making it valuable for research in autoimmune diseases and antiviral responses. Its potency and specificity offer potential for studying the role of TLR7 in various biological contexts. -
TLR7 Agonist
TLR7 Agonist 28 is a potent agonist targeting Toll-like receptor 7 (TLR7), which plays a critical role in the immune response. This compound has demonstrated significant immunostimulatory activity, making it a valuable tool for enhancing antitumor responses when conjugated to monoclonal antibodies (mAbs) for cancer immunotherapy. Its application in research supports the development of innovative therapeutic approaches for oncology. -
TLR4 Inhibitor
M62812 free base acts as a toll-like receptor 4 (TLR4) signal transduction inhibitor. It is effective in suppressing activation of endothelial cells and leukocytes and has demonstrated the ability to prevent lethal septic shock in murine models. This compound is valuable for research applications related to sepsis and its underlying mechanisms. -
TLR4 Agonist
3D-Monophosphoryl Lipid (12,16) free acid is a TLR4 agonist that stimulates the immune response through Toll-like receptor 4 activation. This compound serves as a potent vaccine adjuvant, enhancing the immunogenicity of various vaccine formulations. Its application in research includes the development of improved vaccines and studies of innate immune signaling pathways. -
TLR7 Agonist
TLR7 agonist 29 selectively targets Toll-like receptor 7 (TLR7) with an EC50 of 5.2 nM in human cells and 48.2 nM in mouse cells. This compound effectively activates bone marrow-derived macrophages, enhances myeloid cell activity within the tumor microenvironment, and upregulates the expression of key immune markers such as PD-L1, CD86, and IFN-α. TLR7 agonist 29 can also be utilized as a payload in the synthesis of antibody-drug conjugates (ADCs) for targeted cancer therapies. -
Toll-like Receptor (TLR) Modulator
Guignardone L is a toll-like receptor 3 (TLR3) modulator derived from the endophytic fungus Guignardia mangiferae. This compound exhibits immune-regulating properties by influencing TLR3 signaling pathways, making it valuable for research focused on innate immune responses and inflammation. Its unique biological activity positions Guignardone L as a potential tool in the study of immune modulation and therapeutic applications in autoimmune and infectious diseases. -
TLR7 Agonist
TLR7 Agonist 7, also known as compound IIb-26, functions as an agonist for Toll-like receptor 7 (TLR7) with an EC50 of approximately 4 nM. This compound induces pro-inflammatory cytokine production and enhances immune responses, making it a valuable tool for research in immunology and inflammation. TLR7 Agonist 7 can be utilized in studies exploring antiviral immunity and the modulation of immune responses in various disease models. -
TLR-4 Agonist
α-Glucosyl FP20 sodium is a TLR-4 agonist that functions as a vaccine adjuvant. This compound enhances immune responses by stimulating Toll-like receptor 4, which plays a critical role in the innate immune system. It is widely used in research to investigate vaccine efficacy and the modulation of immune responses.

