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Catalog No.
Product Name
Application
Product Information
Citations
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TLR Inhibitor
TLR2-IN-C29 is an inhibitor of TLR2/1 and TLR2/6 signaling.- Qian-Lu Wang, .et al. , Mol Immunol, 2021, Oct;138:99-109 PMID: 34365196
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TLR4 inhibitor
Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor and plays pivotal role in various inflammatory diseases. -
TLR/SCD inhibitor
E6446 dihydrochloride is a robust antagonist for TLR7 and TLR9, with potential applications in studying harmful inflammatory responses. Additionally, it acts as a significant inhibitor of SCD1 with a KD of 4.61 μM. This compound can notably suppress adipogenic differentiation and liver lipogenesis via the SCD1-ATF3 pathway. Studies have indicated that E6446 dihydrochloride can enhance liver pathology in mice on a high-fat diet, making it a potential candidate for researching non-alcoholic fatty liver disease (NAFLD).
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MD2-TLR4 inhibitor
MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively. -
TLR4 Inhibitor
S enantiomer of TAK-242. TAK-242 (Resatorvid), a small-molecule inhibitor of Toll-like receptor (TLR) 4 signaling. TAK-242 is in treatment of sepsis and septic shock. -
TLR9 Inhibitor
ODN 20844 is a TLR9 inhibitor designed to disrupt Toll-like receptor-mediated immune responses. As a guanine-modified inhibitory oligonucleotide, it specifically targets TLR7 and TLR9, leading to a reduction in immune cell activation. This compound is useful for research applications focused on modulating immune pathways and studying immune-related diseases. The sequence of ODN 20844 is 5'-TCCTGGCGc7GGGAAGT-3'. -
TLR7/TLR8 Inhibitor
BMS905 is a potent dual inhibitor of Toll-like receptors 7 and 8, exhibiting IC50 values of 0.7 nM and 3.2 nM, respectively. This compound effectively inhibits IL-6 production induced by TLR7 or TLR8 activation in both human and mouse whole blood. BMS905 serves as a valuable tool for investigating the role of these receptors in autoimmune diseases, particularly lupus. -
TLR Inhibitor
ODN 24991, a guanine-modified inhibitory oligonucleotide, functions as an inhibitor of Toll-like receptors TLR3, TLR7, and TLR9. By disrupting TLR-mediated immune cell signaling, ODN 24991 serves as a valuable tool for investigating immune responses. The compound is particularly useful in research aimed at understanding the role of these TLRs in inflammation and immune regulation. ODN 24991 sequence: 5'-C-C-T-G-G-C-c7rGm-G-G-G-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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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 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. -
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. -
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. -
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. -
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. -
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. -
TLR4/JNK/NF-κB Inhibitor
TLR4-IN-2 is an inhibitor targeting TLR4, JNK, and NF-κB pathways. It demonstrates anti-inflammatory properties by reducing nitric oxide production in LPS-stimulated RAW264.7 cells, with an IC50 of 23.2 µM. By inhibiting TLR4 expression and diminishing JNK phosphorylation, TLR4-IN-2 effectively suppresses NF-κB activation and the transcription of inflammation-related genes, leading to lower levels of iNOS, COX-2, and various inflammatory mediators. This compound shows potential for investigating therapeutic strategies in inflammatory diseases such as rheumatoid arthritis and other inflammatory disorders. -
TLR Inhibitor
IMG-2005 is a Toll-like receptor (TLR) inhibitor that disrupts TLR signaling by mimicking the Toll/interleukin-1 receptor (TIR) domain of MyD88. This mechanism prevents the homodimerization of MyD88, mitigating damage to tracheal epithelial cells and reducing the onset of pulmonary immune diseases. IMG-2005 is valuable for research into TLR-related pathways and the development of therapeutic strategies for respiratory inflammation. -
TLR7/8 Inhibitor
Enpatoran is a potent and orally active dual inhibitor of Toll-like receptors 7 and 8, exhibiting IC50 values of 11.1 nM and 24.1 nM, respectively, in HEK293 cells. This compound is selective, showing no activity against TLR3, TLR4, or TLR9. Enpatoran effectively blocks both synthetic and natural RNA ligands, demonstrating excellent pharmacokinetic properties in vivo. It is a valuable tool for research focused on modulating innate and adaptive immune responses related to autoimmunity. -
TLR3 Inhibitor
CU-CPT 4a is a selective inhibitor of TLR3 signaling, effectively blocking the downstream pathways activated by the TLR3/dsRNA complex. This compound suppresses the production of pro-inflammatory cytokines, including TNF-α and IL-1β, making it a valuable tool for research into immune responses and inflammation. CU-CPT 4a is suitable for studies focused on modulating TLR3-related signaling pathways in various disease models. -
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. -
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. -
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. -
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. -
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. -
TLR4 inhibitor
TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis. -
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. -
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. -
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.
