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Catalog No.
Product Name
Application
Product Information
Citations
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COX Inhibitor
Ketorolac hydrochloride is a non-steroidal anti-inflammatory drug (NSAID) that acts as a nonselective inhibitor of cyclooxygenase (COX), with IC50 values of 20 nM for COX-1 and 120 nM for COX-2. It is utilized in the study of various ophthalmic conditions, including allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain. Additionally, Ketorolac hydrochloride functions as a DDX3 inhibitor, making it relevant for cancer research applications. -
Neddylation Inhibitor
Keap1-Nrf2-IN-4 is a potent neddylation inhibitor that targets the Keap1-Nrf2 pathway. It exhibits significant anti-proliferative activity against MGC-803 gastric cancer cells, with an IC50 value of 2.55 µM. Additionally, Keap1-Nrf2-IN-4 effectively inhibits cell migration and induces apoptosis in these cancer cells, contributing to tumor growth suppression while exhibiting minimal toxicity. This compound is valuable for research into cancer therapies and the regulation of oxidative stress responses. -
COX Inhibitor
Meloxicam sodium is a selective cyclooxygenase (COX) inhibitor, primarily targeting COX-2 with an IC50 of 0.49 μM while exhibiting a higher IC50 of 36.6 μM for COX-1. This non-steroidal anti-inflammatory agent is capable of crossing the blood-brain barrier, making it suitable for research applications involving central nervous system inflammation and pain management. Meloxicam sodium is widely utilized in studies assessing the efficacy of anti-inflammatory therapies. -
COX-1/2 Inhibitor
Taraxerol acetate is an inhibitor of COX-1 and COX-2, exhibiting IC50 values of 116.3 μM and 94.7 μM, respectively. This compound demonstrates notable anticancer properties and has been shown to induce apoptosis in cancer cells. Taraxerol acetate is valuable for research applications focusing on inflammation, pain relief, and cancer treatment mechanisms. -
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. -
NLRP3 Inflammasome Inhibitor
(rac)-NDT-19795 is a potent inhibitor of the NLRP3 inflammasome, exhibiting an IC50 value of 66 nM in peripheral blood mononuclear cells (PBMCs) and 4.7 μM in Western blot assays. This racemic compound is derived from NT-0796 and possesses carboxylic acid activity, facilitating intracellular conversion. (rac)-NDT-19795 is valuable for investigating the mechanisms of inflammation and neurological disorders. -
NLRP3/AIM2 Inhibitor
NLRP3/AIM2-IN-3 is a selective inhibitor targeting the NLRP3 and AIM2 inflammasomes. This compound exhibits potent inhibitory activity against pyroptosis in THP-1 macrophages induced by LPS and nigericin, demonstrating an IC50 value of 0.077 ± 0.008 μM. NLRP3/AIM2-IN-3 disrupts the interactions between NLRP3 or AIM2 and the adaptor protein ASC, thereby preventing ASC oligomerization and subsequent inflammasome activation. This reagent is suitable for studies investigating inflammasome-mediated processes and pyroptotic cell death. -
NLRP1/3 Inhibitor
ADS032 is a sulfonylurea compound that functions as an inhibitor of the NLRP1 and NLRP3 inflammasomes. This compound effectively reduces the secretion of pro-inflammatory cytokines and inhibits the oligomerization of ASC, thereby exhibiting anti-inflammatory properties. ADS032 can be utilized in various research applications related to inflammatory diseases, making it a valuable tool for studying inflammasome-mediated pathways. -
NLRP3 Inhibitor
Selnoflast (RO7486967) is a highly selective and reversible small molecule inhibitor of the NLRP3 inflammasome. It effectively inhibits the release of IL-1β in response to NLRP3 activation in human monocyte-derived macrophages associated with Alzheimer's disease. Selnoflast is a valuable reagent for research into Alzheimer's disease and systemic inflammatory conditions, including ulcerative colitis and chronic obstructive pulmonary disease. -
AQP9 Inhibitor
RG100204 is a selective inhibitor of the aquaporin 9 (AQP9), targeting its channel function to obstruct the transmembrane transport of water, glycerol, and hydrogen peroxide (H2O2). This compound exhibits significant anti-inflammatory activity by reducing the activation of the NLRP3 inflammasome and the p38 MAPK signaling pathways, leading to decreased inflammation and pyroptosis. In preclinical studies, RG100204 has demonstrated the ability to mitigate multi-organ dysfunction in mouse models of sepsis and has shown potential glucose-regulating effects in diabetic db/db mice. -
NLRP3 Inhibitor
Ruvonoflast is a selective and orally active inhibitor of the NLRP3 inflammasome, effectively penetrating the central nervous system. With an IC50 of 0.32 nM, it inhibits IL-1β release in human peripheral blood mononuclear cells. Upon intracellular conversion to its active carboxylic acid form, Ruvonoflast demonstrates the ability to reverse obesity, systemic inflammation, and astrogliosis in mouse models of diet-induced obesity. This compound holds promise for research into neurodegenerative diseases such as Alzheimer's, Parkinson's, multiple sclerosis, and amyotrophic lateral sclerosis. -
NLRP3 Inflammasome Inhibitor
NP3-253 is a potent NLRP3 inflammasome inhibitor that exhibits oral bioavailability and can penetrate the blood-brain barrier. By acting as a molecular glue, NP3-253 stabilizes the NLRP3 protein in an inactive state, thereby effectively reducing the production of pro-inflammatory cytokines, including IL-1β and IL-18. This compound is valuable for studying inflammatory processes and neurological disorders, such as peritonitis, providing insights into therapeutic strategies for these conditions. -
NLRP3 Inhibitor
AZD4144 is a selective NLRP3 inhibitor with an effective concentration (EC50) of 0.082 μM. This compound significantly reduces the release of IL-1β associated with NLRP3 overactivation, demonstrating pronounced anti-inflammatory properties. With minimal impact on hERG and low cardiotoxicity, AZD4144 serves as a valuable tool for investigating diseases linked to NLRP3 inflammasome activation. -
NLRP3 Inflammasome Inhibitor
(±)11(12)-EET functions as an inhibitor of the NLRP3 inflammasome, playing a significant role in modulating inflammatory processes. This compound demonstrates potential anti-inflammatory, angiogenic, and cardioprotective properties, making it valuable for research aimed at understanding and treating inflammatory diseases and cardiovascular conditions. Its use in preclinical studies can provide insights into the mechanisms underlying these biological activities. -
KCNK13 Inhibitor
CVN293 is a selective inhibitor of the potassium ion channel KCNK13, demonstrating IC50 values of 41 nM and 28 nM for human and mouse KCNK13, respectively. This compound effectively suppresses the NLRP3 inflammasome-mediated production of the proinflammatory cytokine IL-1β in microglial cells. CVN293's brain permeability and targeted action make it a valuable tool for researching neuroinflammatory processes and potential therapeutic interventions. -
Inflammatory Corpuscles Inhibitor
JC2-11 is an inhibitor of inflammatory corpuscles that targets domain-containing proteins NLRC4 and AIM2, as well as non-canonical inflammatory pathways. This compound is effective in reducing the secretion of caspase-1 (p20) and the cleavage of gasdermin D (GSDMD), leading to decreased release of IL-1β and lactate dehydrogenases (LDH) from inflammatory bodies. JC2-11 also disrupts the activation of inflammatory corpuscles by inhibiting reactive oxygen species production and caspase-1 activity, making it a valuable tool for research into inflammation and related diseases. -
NLRP3/AIM2 Inhibitor
NLRP3/AIM2-IN-2 is a selective inhibitor targeting the NLRP3 and AIM2 inflammasomes, demonstrating potent species-specific effects on inflammasome-dependent cell death. With an IC50 value of 0.2392 µM, this compound serves as a valuable tool for investigating the role of NLRP3 and AIM2 in inflammatory processes and cell death pathways. Its use can provide insights into therapeutic strategies for diseases characterized by dysregulated inflammasome activity. -
NLRP3 Inhibitor
BAL-0028 is a reversible inhibitor of the NLRP3 inflammasome, demonstrating an IC50 of 25 nM. This compound selectively binds to the NACHT domain of NLRP3, with KD values ranging from 104 to 123 nM. BAL-0028 effectively inhibits the secretion of IL-1β, exhibiting notable anti-inflammatory properties, making it a valuable tool in research focused on inflammatory diseases and immune responses. -
P2 Receptor Inhibitor
Oxidized ATP trisodium salt is an irreversible antagonist of P2 receptors, particularly effective against P2X7R activation. This compound has been shown to inhibit c-reactive protein (CRP)-induced activation of the NLRP3 inflammasome, thereby modulating inflammatory responses. Oxidized ATP trisodium salt is a valuable tool for research applications related to atherosclerosis and other inflammatory conditions. -
NLRP3 Inflammasome Inhibitor
NDT-19795 is a potent inhibitor of the NLRP3 inflammasome, demonstrating an IC50 value of 66 nM in peripheral blood mononuclear cells (PBMC) and 4.7 μM in Western blot assays. This carboxylic acid-active compound is an active metabolite of NT-0796, contributing to its efficacy within cellular contexts. NDT-19795 is applicable in research focused on inflammatory pathways and neurological disorders, providing valuable insights into the modulation of the NLRP3 inflammasome. -
Potassium Channel Inhibitor
DPO-1 is a selective inhibitor of Kv1.5 and Kv1.3 potassium channels (EC50 = 3.1 μM) with notable immunomodulatory and anti-inflammatory properties. It effectively reduces Kv1.3 current density, diminishes Ca2+ influx in calcium-depleted Jurkat cells, and inhibits IL-2 secretion in activated Jurkat cells. Additionally, DPO-1 obstructs uric acid sodium (MSU)-induced NLRP3 inflammasome activation by interfering with Kv1.5-mediated K+ efflux. This reagent is valuable for research into immunological disorders and atrial fibrillation. -
NLRP3 Inhibitor
JT002 is a selective inhibitor of the NLRP3 inflammasome assembly. It effectively reduces the production of NLRP3-dependent proinflammatory cytokines, including IL-1β, IL-1α, and IL-18, while also inhibiting pyroptosis. In preclinical studies, JT002 demonstrated the ability to mitigate airway hyperresponsiveness and airway neutrophilia in murine models, making it a valuable tool for investigating various inflammatory diseases, such as Muckle-Wells syndrome. -
NLRP3 Inhibitor
NLRP3-IN-13 is a selective and potent inhibitor of the NLRP3 inflammasome, exhibiting an IC50 value of 2.1 μM. This compound effectively inhibits both NLRP3 and NLRC4 inflammasome activity, as well as NLRP3-mediated interleukin-1 beta (IL-1β) production. Additionally, NLRP3-IN-13 disrupts NLRP3 ATPase activity, making it a valuable tool for investigating neuroinflammatory disorders and related pathways. -
NLRP3 Inhibitor
JC124 is a selective inhibitor of the NLRP3 inflammasome, a crucial component in the inflammatory response. It demonstrates significant anti-inflammatory activities and provides neuroprotective effects, making it a valuable tool in research aimed at understanding neuroinflammation and related disorders. JC124 is suitable for studies investigating the modulation of inflammatory pathways and potential therapeutic interventions in various neurological conditions. -
NLRP3 Inhibitor
INF 195 is a potent NLRP3 inhibitor that effectively suppresses NLRP3-driven macrophage pyroptosis and interleukin-1 beta (IL-1β) release, exhibiting an EC50 value of 0.15 μM. This compound has demonstrated the ability to reduce infarct size in isolated mouse hearts at low doses, thereby providing protection against myocardial ischemia/reperfusion injury. INF 195 serves as a valuable tool for research focused on inflammation and cardiovascular diseases.
