Catalog No.
Product Name
Application
Product Information
Citations
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Antibiotic Agent
Cloxacillin sodium is a β-lactam antibiotic and a potent β-lactamase inhibitor with an IC50 of 0.04 µM. It exhibits significant antibacterial activity, particularly against Staphylococcus aureus, and can effectively attenuate the S. aureus-induced inflammatory response by inhibiting the activation of MAPK, NF-κB, and NLRP3-related proteins. This compound is relevant for research in antimicrobial resistance and inflammation pathways. -
Drd2 Agonist
UNC9995 is a β-arrestin2-biased agonist of the dopamine receptor Drd2. This compound inhibits NLRP3 inflammasome activation by promoting the interaction between β-arrestin2 and NLRP3, thereby preventing neuronal degeneration. Furthermore, UNC9995 activates Drd2/β-arrestin2 signaling, which mitigates the transcription of inflammation-related genes induced by the JAK/STAT3 pathway. Research shows that UNC9995 enhances depressive behavior in mouse models and improves astrocyte dysfunctions, making it a valuable tool for studying neuroinflammatory processes and mood disorders. -
Pyroptosis Inducer
PenCB (PCB 118) is a potent pyroptosis inducer that primarily activates the NFκB-dependent NLRP3 inflammasome pathway. Its mechanism involves the induction of oxidative stress, which is mediated through the activation of the aryl hydrocarbon receptor (AhR) and subsequent upregulation of cytochrome P450 1A1. This compound is useful for studies examining inflammatory processes and cell death mechanisms, particularly in the context of pyroptosis-related research. -
Pyroptosis Inhibitor
Azalamellarin N is a selective inhibitor of pyroptosis, effectively modulating the inflammatory response by targeting upstream signaling pathways involved in NLRP3 inflammasome activation. This compound exhibits differential inhibitory effects on various pyroptosis inducers, with notable potency against Nigericin and R837. Its mechanism provides a valuable tool for investigating the role of pyroptosis in cellular processes and disease states, making it significant for research in inflammation and immune responses. -
NLRP3 Inhibitor
NLRP3-IN-78 is a potent inhibitor of the NLRP3 inflammasome, demonstrating a 46.72% inhibition rate in GSDMD-induced pyroptosis at a concentration of 5 μM. This compound effectively binds to the NLRP3 protein, hindering GSDMD-NT oligomerization and cleavage while also suppressing upstream NF-κB signaling. NLRP3-IN-78 serves as a valuable tool for investigating anti-inflammatory mechanisms and the role of NLRP3 in various disease models. -
Drug Metabolite
Carvedilol Glucuronide is a significant metabolite of the β/α-1 adrenergic receptor antagonist, Carvedilol. This compound demonstrates key biological activity by modulating β-adrenergic signaling and exhibits potential application in studying the metabolic pathway of Carvedilol. Research indicates that Carvedilol can inhibit lipid peroxidation and has properties as an antihypertensive agent, as well as an autophagy inducer that affects the NLRP3 inflammasome. Carvedilol Glucuronide serves as an important reagent for investigating drug metabolism and pharmacokinetics in cardiovascular research. -
NEK7 Molecular Glue Degrader
NEK7 degrader-3 is an orally active NEK7 molecular glue degrader with a DC50 of 33.1 nM, which effectively mediates the interaction between NEK7 and the E3 ligase cereblon, leading to the proteasomal degradation of NEK7. This degradation process attenuates NLRP3 inflammasome-mediated inflammatory responses, resulting in the inhibition of caspase-1 activity and the release of pro-inflammatory cytokines IL-1β, IL-1α, and IL-18. NEK7 degrader-3 demonstrates significant anti-inflammatory effects in LPS-induced neuroinflammation mouse models, serving as a valuable tool for research focused on neuroinflammation. -
Anti-inflammatory Agent
MBL-1 is an orally active anti-inflammatory agent that targets the hCOX-2 protein, demonstrating an IC50 of 5.77 μM. This compound effectively reduces the production of key pro-inflammatory mediators, including nitrogen oxide (NO), reactive oxygen species (ROS), IL-1β, and IL-18, by inhibiting the MAPK/NF-κB and NLRP3 signaling pathways. MBL-1 has shown protective effects against dextran sulfate sodium (DSS)-induced colitis, making it a valuable tool for research into ulcerative colitis and related inflammatory conditions. -
IDE/NLRP3 Inhibitor
ML345 is a selective inhibitor of insulin-degrading enzyme (IDE) and NLRP3, exhibiting an IC50 of 188 nM for IDE. By targeting the Cys819 residue, ML345 effectively inhibits IDE activity, while it binds non-covalently to NLRP3, modulating its function. This compound is known to inhibit the release of inflammatory cytokines such as IL-1β and IL-6, demonstrating significant anti-inflammatory properties. Additionally, ML345 has been shown to provide protective effects against miscarriage, making it a valuable tool for research in inflammation and reproductive health. -
Fas receptor Antagonist
Xelafaslatide is a Fas receptor antagonist that effectively inhibits Fas receptor signaling, thereby blocking downstream apoptosis and inflammatory pathways. This compound demonstrates significant potential in suppressing neuroinflammation and microglial activation in glaucoma models, offering protection to retinal ganglion cells and preventing axonal degeneration. Xelafaslatide is relevant for research focused on glaucoma and related neurodegenerative conditions. -
HDAC3 Degrader
HDAC3 Degrader-2 is a selective degrader of histone deacetylase 3 (HDAC3), functioning through targeted degradation to inhibit the activation of the NLRP3 inflammasome. By facilitating the reduction of IL-1β maturation and caspase-1 activity, HDAC3 Degrader-2 demonstrates significant anti-inflammatory effects. This reagent is applicable in researching conditions such as endotoxin shock, colitis, and gouty arthritis, providing valuable insights into mechanisms of inflammation and therapeutic interventions. -
P2Y12 Receptor Activator
ADP-β-S trilithium is the trilithium salt form of ADP-β-S, serving as a potent activator of the P2Y12 receptor. It facilitates the upregulation of IL-1β and IL-6 production in microglial cells, promotes NF-κB phosphorylation and nuclear translocation, and enhances NLRP3 inflammasome activation. This reagent is valuable for research into inflammatory responses and signaling pathways involving P2Y12 receptor activation. -
NOD1 inhibitor
Nodinitib-1 (ML130;CID-1088438) is a NOD1 inhibitor with an IC50 of 0.56 μM. -
NLRP3 inflammasome inhibitor
Dapansutrile (OLT1177) is a potent, selective and orally active inhibitor of NLRP3 inflammasome. Anti-inflammatory, analgesic activity. -
Anti-cancer Agent
Dihydromethysticin is a naturally occurring compound primarily targeting carboxylesterase 1 and CYP2A5. This orally active agent has demonstrated the ability to upregulate NLRC3 and induce apoptosis, showcasing its potential as an anti-cancer agent. Research indicates that dihydromethysticin exhibits significant anticancer activity against colorectal cancer and lung adenoma, making it a valuable tool in cancer research and therapeutic development. -
Cardioprotective Agent
Kanglexin is a novel anthraquinone compound that acts as a cardioprotective agent by inhibiting NLRP3 inflammasome activation and cell pyroptosis. This compound promotes angiogenesis through the FGFR1/ERK signaling pathway and enhances diabetic wound healing. Additionally, Kanglexin exhibits lipid-lowering effects and inhibits the dedifferentiation of vascular smooth muscle cells, making it a valuable tool for researching hyperlipidemia, fatty liver disease, and atherosclerosis. -
Stable Isotope
Carvedilol-d3 is a deuterium-labeled analogue of Carvedilol, functioning primarily as a non-selective β/α-1 adrenergic receptor blocker. It exhibits significant biological activity by inhibiting lipid peroxidation in a dose-dependent manner with an IC50 value of 5 μM. This compound serves as a versatile antihypertensive agent and has potential applications in the treatment of angina and congestive heart failure. Furthermore, Carvedilol-d3 promotes autophagy and is known to inhibit the NLRP3 inflammasome, making it valuable for research involving inflammatory processes. -
Stable Isotope
Carvedilol-d5 is a deuterium-labeled analogue of Carvedilol, a non-selective β/α-1 adrenergic receptor blocker. It exhibits lipid peroxidation inhibition with an IC50 of 5 μM and serves as a versatile antihypertensive agent, showing potential in the treatment of angina and congestive heart failure. Additionally, Carvedilol functions as an autophagy inducer and inhibits the NLRP3 inflammasome, making it relevant for research in inflammatory pathways and cardiovascular health. -
Antioxidant
Dihydrolipoic Acid (DHLA) is a potent antioxidant primarily targeting reactive oxygen species. It demonstrates significant anti-inflammatory effects across various disease models. Research indicates that DHLA can modulate the ERK/Nrf2/HO-1/ROS/NLRP3 signaling pathway, effectively mitigating sickness behavior in LPS-induced rat models. This compound is valuable for studies related to depression and oxidative stress-related disorders. -
Stable Isotope
Carvedilol-d4 is a deuterated derivative of Carvedilol, a non-selective β/α-1 adrenergic receptor antagonist. It exhibits dose-dependent inhibition of lipid peroxidation with an IC50 value of 5 μM. Carvedilol acts as a multifaceted antihypertensive agent, demonstrating potential therapeutic applications in managing conditions such as angina and congestive heart failure. Additionally, it has been identified as an autophagy inducer and a modulator of the NLRP3 inflammasome, making it a valuable tool for research into cardiovascular and inflammatory diseases. -
Stable Isotope
Stavudine-d4 is a deuterium-labeled derivative of Stavudine, a potent nucleoside reverse transcriptase inhibitor (NRTI) targeting HIV-1 and HIV-2. This stable isotope is utilized in research applications to study metabolic processes and pharmacokinetics of Stavudine while minimizing background signal from natural isotopes. In addition, Stavudine is known to affect mitochondrial DNA replication, reduce NLRP3 inflammasome activation, modulate Amyloid-β autophagy, and induce apoptosis, making it a valuable tool for investigations into viral pathogenesis and cellular mechanisms. -
Nucleoside Reverse Transcriptase Inhibitor
Stavudine sodium is a nucleoside reverse transcriptase inhibitor (NRTI) primarily utilized for its efficacy against HIV-1 and HIV-2. This compound demonstrates the ability to inhibit mitochondrial DNA replication, reduce NLRP3 inflammasome activation, and modulate the autophagy of Amyloid-β, contributing to its therapeutic potential. Additionally, Stavudine sodium is associated with inducing apoptosis in targeted cells, making it a valuable tool in HIV research and related cellular studies. -
R-isomer of Colchicine
(R)-Colchicine is the R-isomer of Colchicine, a potent inhibitor of tubulin polymerization. It exhibits a strong microtubule-disruptive mechanism, with an IC50 value of 3 nM. In addition to its role as a tubulin inhibitor, (R)-Colchicine acts as a competitive antagonist of the α3 glycine receptors, contributing to its diverse biological activities. This compound is significant in research focused on anti-inflammatory responses, immunosuppression, and treatment strategies for gouty arthritis, particularly by mitigating NSAID-induced intestinal injury through NLRP3 inflammasome inhibition. -
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. -
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. -
Antacid Aegnt
Aluminum Hydroxide is a well-known antacid agent that functions primarily as an adjuvant in vaccine formulations. It enhances the immune response by promoting the pro-phagocytic effect and activating the pro-inflammatory NLRP3 pathway. Additionally, Aluminum Hydroxide compensates for the low immunogenicity often associated with subunit vaccines, making it a valuable component in immunological research and development. -
Immunoreactive Peptide
Muramyl dipeptide (MDP) is a synthetic immunoreactive peptide that targets NLRP1 and plays a significant role in bone formation. It induces osteoblast differentiation by up-regulating Runx2 gene expression via MAPK signaling pathways. Muramyl dipeptide is widely utilized in research focused on bone metabolism and immunological responses. -
ROS/NLRP3 Inflammasome Activator
Trimethylamine N-oxide is a gut microbiome-derived metabolite that primarily activates the ROS/NLRP3 inflammasome, leading to inflammatory responses. Its biological activity extends to promoting fibroblast-myofibroblast differentiation and inducing cardiac fibrosis through the TGF-β/smad2 signaling pathway. These properties make Trimethylamine N-oxide a valuable reagent for research into inflammation, fibrosis, and the interplay between dietary components and immune responses. -
NLRP3 Agonist
BMS-986299 is a first-in-class NLRP3 inflammasome agonist that exhibits potent activation with an EC50 of 1.28 μM. This compound is valuable for research exploring the role of NLRP3 in inflammatory processes and immune responses. Its ability to selectively stimulate the NLRP3 pathway makes it an important tool for studies related to autoinflammatory diseases and the development of novel immunotherapeutic strategies. -
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. -
NLRP3 Activator
QS-21-Api is a potent NLRP3 activator that functions as an immunostimulatory saponin, enhancing vaccine efficacy as an adjuvant. It stimulates both Th2 humoral and Th1 cell-mediated immune responses by acting on antigen presenting cells (APCs) and T cells. Through the activation of the NLRP3 inflammasome, QS-21-Api prompts the release of caspase-1 dependent cytokines, including IL-1β and IL-18, making it a valuable tool for research in immunology and vaccine development. -
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. -
Endogenous Metabolite
Desmosterol is a cholesterol precursor involved in the Bloch pathway of cholesterol biosynthesis. As an endogenous metabolite, it plays a critical role in the study of cholesterol metabolism. Desmosterol functions as a liver X receptor (LXR) activator and SREBP inhibitor, which can mitigate macrophage inflammasome activation, thereby reducing vascular inflammation and the risk of atherosclerosis. Furthermore, lower levels of Desmosterol can lead to increased production of mitochondrial reactive oxygen species (ROS) in macrophages and activate the NLRP3 inflammasome through pyrin domain mechanisms. This compound is valuable for research focused on inflammation, metabolic processes, and cardiovascular diseases. -
ROS/NLRP3 Inflammasome Activator
Trimethylamine N-oxide dihydrate is an activator of the ROS/NLRP3 inflammasome, functioning as a gut microbe-derived metabolite of dietary choline and other trimethylamine-rich nutrients. This compound promotes inflammatory responses and plays a role in the differentiation of fibroblasts to myofibroblasts, thereby contributing to cardiac fibrosis through the activation of the TGF-β/smad2 signaling pathway. Its properties make it valuable in studies focused on inflammation and fibrosis mechanisms in various biological contexts. -
Stable Isotope
Trimethylamine N-oxide-d9 is a deuterium-labeled form of Trimethylamine N-oxide, a gut microbiome-dependent metabolite derived from dietary choline and trimethylamine-rich nutrients. This compound has been shown to induce inflammation through the activation of the ROS/NLRP3 inflammasome. Additionally, Trimethylamine N-oxide is involved in accelerating fibroblast-to-myofibroblast differentiation, promoting cardiac fibrosis via the TGF-β/smad2 signaling pathway. It is a valuable reagent for research on metabolic disorders and cardiovascular diseases. -
NLRX1 Activator
Amelenodor is an NLRX1 activator that induces immunometabolic changes by selectively targeting the NLRX1 pathway. This compound demonstrates potential in reducing inflammation and modulating immune responses in inflammatory bowel diseases. Research applications include studies on Crohn's disease and ulcerative colitis, making it a valuable tool for advancing understanding of these conditions. -
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.
