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NOD-like receptors inhibitor
NOD-IN-1 is a potent mixed inhibitor of nucleotide-binding oligomerization domain (NOD)-like receptors, NOD1 and NOD2, with IC50 of 5.74 μM and 6.45 μM, respectively.- Shuqin Lai, .et al. , Int Immunopharmacol, 2025, Feb 6:147:114036 PMID: 39778279
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NLRP3 inhibitor
MCC950 sodium is a potent NLRP3 inflammasome inhibitor that inhibits IL-1beta production with IC50 value of 7.5 nm.- Takemasa Takii, .et al. , mSphere, 2025, 10:e00110-25 PMID: 40387341
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NLRP3 inflammasome inhibitor
Isoliquiritigenin is a licorice chalconoid, a type of natural phenols that is currently under experimentation phase testing for use as a cancer treatment as well as an aide for cocaine addiction. -
TNF Receptor Inhibitor
Muscone, a TNF receptor inhibitor, is derived from the traditional Chinese medicine musk. It effectively inhibits NF-κB signaling and NLRP3 inflammasome activation, resulting in a significant reduction of inflammatory cytokines such as IL-1β, TNF-α, and IL-6. This compound is valuable in research focused on inflammation, cardiac function restoration, and improving survival rates in various pathological conditions. -
NLRP3 Inhibitor
Tabersonine hydrochloride is a selective NLRP3 inhibitor that targets the NACHT domain of the NLRP3 protein, effectively inhibiting its ATPase activity and oligomerization. This action prevents ASC spot formation and caspase-1 activation, leading to a reduction in pro-inflammatory cytokine release, including IL-1β. Additionally, Tabersonine hydrochloride inhibits K63-linked ubiquitination of TRAF6, interfering with NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Its applications extend to the study of NLRP3-driven inflammatory conditions, such as acute lung injury, sepsis, and peritonitis, as well as in liver cancer research, where it induces apoptosis through mitochondrial and death receptor pathways. -
Pyroptosis Inhibitor
7-Oxogedunin is a potent inhibitor of pyroptosis, acting primarily on protein kinase R (PKR). It effectively protects macrophages from cell death induced by anthrax lethal toxin and inhibits the assembly of various inflammasomes, including NLRP1 and NLRP3, as well as the activation of caspase-1 through its effects on PKR. In addition to its role in cell survival, 7-Oxogedunin exhibits growth inhibitory activity against European corn borer larvae, making it valuable for research in LT toxicity and pest control. -
NLRP3 Inhibitor
NLRP3-IN-81 is a potent inhibitor targeting the NLRP3 inflammasome, effectively preventing NLRP3-dependent pyroptosis with an EC50 of 0.029 μM in cell models using Nigericin. This compound inhibits the activation of caspase-1 and the subsequent release of IL-1β by disrupting the interaction between NLRP3 and the adaptor protein ASC, thereby inhibiting ASC oligomerization. NLRP3-IN-81 is relevant for research into pyroptosis-related conditions, including inflammatory bowel diseases and type 2 diabetes. -
NLRP3 Inhibitor
NLRP3-IN-87 is a selective, orally active inhibitor of the NLRP3 inflammasome, exhibiting a Kd value of 0.23 μM. This compound directly targets the NACHT domain of NLRP3, effectively disrupting its interactions with NEK7 and ASC, thereby inhibiting ASC oligomerization and inflammasome assembly. NLRP3-IN-87 is known to suppress caspase-1 activation and IL-1β secretion, demonstrating significant anti-inflammatory and analgesic effects. It is particularly useful for investigating the pathophysiology of gout as it reduces joint swelling, inflammation, and pain in MSU-induced acute gout models. -
NLRP3 Inflammasome Inhibitor
NP3-146 sodium is a selective inhibitor of the NLRP3 inflammasome, effectively binding to the NACHT domain of NLRP3. This compound demonstrates significant inhibition of IL-1β release, achieving an IC50 value of 0.171 μM in LPS/Nigericin-stimulated bone marrow-derived macrophages (BMDM). NP3-146 sodium modulates the levels of cleaved Caspase-1 and cleaved IL-1β in cell supernatants, making it a valuable tool for research into inflammatory diseases. -
NLRP3 Inhibitor
GDC-2394 sodium is a selective NLRP3 inhibitor that exhibits potent activity against IL-1β, with IC50 values of 0.4 μM for human IL-1β and 0.1 μM for mouse IL-1β. This compound effectively inhibits NLRP3-induced caspase-1 activity while leaving NLRC4-dependent inflammasome activation unaffected. GDC-2394 sodium is particularly relevant for research into gouty arthritis and may serve as a valuable tool in the study of inflammatory diseases linked to NLRP3 activation. -
NLRP3 Inhibitor
NP3-146 is a potent inhibitor of the NLRP3 inflammasome, acting by locking the NACHT domain of NLRP3. It effectively reduces IL-1β release, with an IC50 value of 0.171 μM in LPS/Nigericin-stimulated bone marrow-derived macrophages (BMDM). Additionally, NP3-146 modulates the levels of cleaved Caspase-1 and cleaved IL-1β in cell supernatants, making it a valuable tool in the study of inflammatory diseases. -
NLRP3 Inhibitor
GDC-2394 is a selective NLRP3 inhibitor that acts orally, demonstrating inhibitory effects on IL-1β with IC50 values of 0.4 μM for human IL-1β and 0.1 μM for mouse IL-1β. This compound effectively inhibits NLRP3-induced caspase-1 activity while sparing NLRC4-dependent inflammasome activation. GDC-2394 is valuable for research into inflammatory conditions such as gouty arthritis. -
NLRP3 Inhibitor
1,2,4-Trimethoxybenzene is a selective inhibitor of the NLRP3 inflammasome, exerting its effects orally. It significantly suppresses NLRP3 activation induced by Nigericin or ATP, leading to reduced caspase-1 activation and IL-1β secretion. This compound specifically targets the NLRP3 inflammasome without influencing AIM2 inflammasome activation, and it prevents the oligomerization of ASC and the interaction between NLRP3 and ASC, thus inhibiting inflammasome assembly. 1,2,4-Trimethoxybenzene is valuable for researching autoimmune disorders such as experimental autoimmune encephalomyelitis, multiple sclerosis, and metabolic conditions like type 2 diabetes. -
NLRP3 Inhibitor
Tabersonine is a selective and orally active inhibitor of the NLRP3 inflammasome, targeting the NACHT domain to modulate its ATPase activity and prevent oligomerization. This mechanism effectively inhibits ASC speck formation and blocks caspase-1 activation, leading to reduced secretion of pro-inflammatory cytokines, including IL-1β. Additionally, Tabersonine interferes with K63-linked ubiquitination of TRAF6, disrupting NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. It is primarily utilized in research on NLRP3-mediated inflammatory diseases, such as acute lung injury, sepsis, and peritonitis, as well as in studies related to liver cancer. -
PCSK9 Inhibitor
Inclisiran is a double-stranded small interfering RNA (siRNA) that specifically targets and inhibits the transcription of proprotein convertase subtilisin/kexin type 9 (PCSK9). By reducing PCSK9 levels, Inclisiran effectively modulates lipid metabolism and demonstrates anti-inflammatory properties, including the inhibition of pyroptosis and a decrease in NLRP3, cleaved caspase-1, IL-1β, and IL-18. This reagent is valuable for research applications focused on hyperlipidemia and cardiovascular diseases (CVD), as it supports studies aimed at understanding lipid regulation and atherosclerosis. -
NLRP3 Inhibitor
Magnesium isoglycyrrhizinate hydrate is a potent NLRP3 inflammasome inhibitor derived from the licorice plant (Glycyrrhiza glabra). It displays significant anti-inflammatory properties, making it a valuable compound for research into inflammatory diseases. Its efficacy in attenuating conditions such as chronic obstructive pulmonary disease in preclinical rat models highlights its potential applications in respiratory research and therapeutic development. -
Autophagy Inducer, NLRP3 Inhibitor
Britannin is an autophagy inducer and NLRP3 inflammasome inhibitor with an IC50 of 3.630 μM. It exhibits significant anti-inflammatory effects by disrupting the interaction between NLRP3 and NEK7, effectively preventing NLRP3 activation and assembly. Additionally, Britannin shows antitumor properties by inhibiting tumor cell proliferation through interference with the interaction of HIF-1α and Myc, leading to reduced PD-L1 expression and enhanced activity of cytotoxic T lymphocytes. This compound also promotes apoptosis and autophagy in liver cancer cells via activation of ROS-regulated AMPK, making it a valuable tool for research in anti-inflammatory and oncology studies. -
ACE/IKK-β/PKC Inhibitor
Plantainoside D is a phenylethanoid glycoside that functions primarily as an inhibitor of IKK-β, with additional inhibitory effects on angiotensin-converting enzyme (ACE) and protein kinase C (PKC). It exhibits significant biological activities, including the reduction of glutamate release in the rat cerebral cortex, alleviating cell apoptosis through the inhibition of reactive oxygen species (ROS) and NF-κB activation. Additionally, Plantainoside D has been shown to improve outcomes in acute lung injury induced by sepsis via modulation of the Sirt3/NLRP3 signaling pathway. This compound is applicable in studies of neuroprotection, antioxidant activity, anti-inflammatory responses, and antihypertensive effects. -
TREM-1 Inhibitor
Nangibotide is a synthetic peptide that serves as a TREM-1 receptor inhibitor. By inhibiting NF-κB and NLRP3 inflammasome activation, Nangibotide effectively reduces the release of pro-inflammatory cytokines such as IL-1β and IL-8 and mitigates apoptosis. This reagent is valuable for research applications related to excessive inflammatory responses, including studies on myocardial ischemia-reperfusion injury, septic shock, acute lung injury, osteoarthritis, and acute liver failure. Additionally, Nangibotide offers protective effects on tissues, such as the liver and lung, during inflammatory conditions. -
PDE IV Inhibitor/A1AR Antagonist
Doxofylline is an orally active phosphodiesterase IV (PDE IV) inhibitor and adenosine A1 receptor (A1AR) antagonist. It exhibits anti-inflammatory properties by reducing mitochondrial reactive oxygen species (ROS) production and modulating various cellular pathways, including the NLRP3-TXNIP inflammasome activation. This compound is valuable for research related to respiratory diseases such as asthma, chronic obstructive pulmonary disease (COPD), and bronchospasm. -
Nox2 Inhibitor
gp91 ds-tat is a specific inhibitor of NADPH oxidase 2 (Nox2), effectively blocking the production of superoxide generated by this enzyme. This bioactive peptide has demonstrated the ability to reduce reactive oxygen species (ROS), lipid peroxidation, and iron levels induced by high glucose conditions. Additionally, gp91 ds-tat inhibits homocysteine-induced activation of NLRP3 inflammasomes and restores the activity of lysosomal TRPML1 channels. Research applications include studies on Alzheimer's disease, glomerular inflammation, and cardiovascular disease, with implications for improving cerebrovascular and cognitive functions in APP/PS1 mouse models. -
Nucleoside Reverse Transcriptase Inhibitor
Stavudine is an orally active nucleoside reverse transcriptase inhibitor (NRTI) that selectively targets HIV-1 and HIV-2. In addition to its antiviral properties, Stavudine inhibits mitochondrial DNA replication and has been shown to reduce NLRP3 inflammasome activation while modulating Amyloid-β autophagy. Furthermore, Stavudine is associated with the induction of apoptosis, making it a valuable tool for research in HIV treatment and cellular apoptosis mechanisms. -
CYP51/PD-L1 Inhibitor
CYP51/PD-L1-IN-3 is a dual inhibitor targeting CYP51 and PD-L1, exhibiting potent antifungal activity with IC50 values of 0.205 μM and 0.039 μM, respectively. This compound induces early apoptosis in fungal cells by reducing levels of intracellular IL-2, NLRP3, and NF-κBp65 proteins. Additionally, CYP51/PD-L1-IN-3 causes mitochondrial damage and reactive oxygen species (ROS) accumulation, ultimately resulting in fungal lysis and cell death. This compound serves as a valuable tool for research in fungal infections and immune modulation. -
CYP51/PD-L1 Inhibitor
CYP51/PD-L1-IN-2 is a quinazoline compound that functions as a dual inhibitor of CYP51 and PD-L1, exhibiting IC50 values of 0.263 μM and 0.017 μM, respectively. It displays notable antifungal activity by triggering early apoptosis in fungal cells, leading to significant reductions in intracellular IL-2, NLRP3, and NF-κBp65 protein levels. Additionally, CYP51/PD-L1-IN-2 induces mitochondrial damage and reactive oxygen species (ROS) accumulation, culminating in fungal lysis and subsequent cell death. This compound is valuable for research exploring antifungal mechanisms and cancer immunotherapy. -
CYP51/PD-L1 Inhibitor
CYP51/PD-L1-IN-1 is a dual inhibitor targeting both CYP51 and PD-L1, exhibiting an IC50 of 0.884 μM for CYP51 and 0.083 μM for PD-L1. This quinazoline compound demonstrates notable antifungal activity by inducing early apoptosis in fungal cells while significantly reducing intracellular levels of IL-2, NLRP3, and NF-κBp65. Additionally, CYP51/PD-L1-IN-1 contributes to mitochondrial damage and reactive oxygen species (ROS) accumulation, ultimately leading to fungal lysis and cell death. This compound is valuable for research focused on antifungal therapies and immune modulation. -
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. -
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. -
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. -
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. -
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.

