Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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.
