NOD-like Receptor (NLR)

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  1. NOD-like Receptor (NLR) Inhibitor

    NLRP3-IN-4 is a potent inhibitor of the NOD-like receptor (NLR) NLRP3 inflammasome, exhibiting oral bioavailability. This compound is characterized by its ability to mitigate inflammatory processes, making it particularly relevant for research in inflammatory diseases such as colitis. It is a valuable tool for investigating the role of NLRP3 in immune responses and inflammation modulation.
  2. NLRP3 Inhibitor

    NLRP3-IN-64 is a selective inhibitor of the NLRP3 inflammasome, exhibiting an EC50 of 5 nM for the inhibition of NLRP3 activation. This compound is useful for investigating the role of NLRP3 in inflammatory diseases and provides a valuable tool for research in immune response modulation. Its application extends to studying the mechanisms underlying autoinflammatory conditions and potential therapeutic interventions.
  3. NLRP3 Inhibitor

    Sebrinoflast is a potent NLRP3 inhibitor, exhibiting an IC50 of ≤1 μM for human NLRP3. This compound is valuable in the study of inflammatory conditions and cardiovascular diseases such as non-alcoholic steatohepatitis (NASH) and atherosclerosis. Additionally, it serves as an important tool in neurological disease research, particularly for Alzheimer's disease.
  4. NLRP3 Inflammasome Inhibitor

    NT-0527 is a selective inhibitor of the NLRP3 inflammasome, demonstrating oral bioavailability and effective permeability across the blood-brain barrier. This compound specifically prevents NLRP3 inflammasome formation, leading to decreased maturation and secretion of interleukin-1 beta (IL-1β). NT-0527 exhibits notable anti-inflammatory effects in models of acute inflammation, including the LPS/ATP-induced peritonitis model. It is a valuable tool for research into neuroinflammatory conditions, such as Parkinson's disease and Alzheimer's disease, as well as peripheral inflammatory disorders like type II diabetes and atherosclerosis involving the NLRP3 pathway.
  5. NOD-like Receptor (NLR) Inhibitor

    GSK223 is a quinazolinone compound that acts as a selective inhibitor of the NOD1 pathway. It demonstrates potential anti-inflammatory activity by selectively inhibiting IL-8 release in response to iE-DAP stimulation, while leaving IL-8 secretion unaffected from TNF receptor, TLR2, or NOD2 agonists. Additionally, GSK223 does not directly inhibit RIP2 kinase activity, making it a valuable tool for studying NOD-like receptor signaling and its implications in inflammatory responses.
  6. NOD-like Receptor (NLR) Inhibitor

    NLRP3-IN-53 is a potent inhibitor of the NOD-like receptor NLRP3, exhibiting an IC50 of 3.4 nM. This compound is utilized in research to investigate the roles of the NLRP3 inflammasome in various inflammatory diseases and immune responses. Its selective inhibition helps elucidate the mechanistic pathways involved in NLRP3-related signaling, making it a valuable tool for studying therapeutic targets in the context of autoimmunity and metabolic disorders.
  7. NLRP3 Inhibitor

    NLRP3-IN-58 is a potent inhibitor of the NLRP3 inflammasome, demonstrating an IC50 value of 3.85 μM. At a concentration of 10 μM, it effectively reduces IL-1β release by 33%. This compound is valuable for research applications focused on inflammatory pathways and the modulation of innate immune responses.
  8. NLRP3 Inhibitor

    NLRP3-IN-56 is a potent inhibitor of the NLRP3 inflammasome, effectively suppressing IL-1β secretion in THP-1 cells with an IC50 of 9.7 nM. This compound serves as a valuable tool for investigating NLRP3-mediated inflammatory responses and associated pathologies. Its ability to modulate IL-1β levels makes it suitable for research into diseases characterized by NLRP3 activation.
  9. NLRP3 Inhibitor

    NLRP3-IN-28 is a potent inhibitor of the NLRP3 inflammasome, demonstrating an EC50 of 0.07 μM in the inhibition of Nigericin-induced pyroptosis. This compound effectively reduces inflammatory responses in vivo, making it a valuable tool for investigating NLRP3-related diseases and inflammatory pathways. Its application in research provides insights into therapeutic strategies targeting inflammasome activation and related inflammatory conditions.
  10. Inflammasome Inhibitor

    3-Et-3TC is a potent inhibitor of the NLRP3 inflammasome, demonstrating its capacity to modulate inflammasome activation. This compound is valuable for investigating the underlying mechanisms of retinal degenerative diseases and other inflammatory conditions. Its structural modification from Lamivudine enhances its efficacy in biochemical research applications targeting inflammasome pathways.
  11. 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.
  12. NLRP3 inhibitor

    MCC950 (CP-456773, CRID3) is a potent and selective inhibitor of NLRP3 (NOD-like receptor (NLR) family, pyrin domain-containing protein 3) with IC50 of 7.5 nM and 8.1 nM in BMDMs and HMDMs, respectively.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. P2X4 Inhibitor

    NP-1815-PX sodium is a selective inhibitor targeting the P2X4 receptor, exhibiting an IC50 of 0.26 μM against human P2X4 receptors. This compound effectively inhibits ATP-mediated prostaglandin production and attenuates TP receptor-induced calcium elevation, as well as NLRP3 inflammasome signaling. Notably, NP-1815-PX sodium demonstrates anti-allodynic effects in vivo and alleviates DNBS-induced colitis symptoms, including weight loss and tissue damage, through the downregulation of IL-1β levels and Caspase-1 activity. This reagent is applicable in research areas such as asthma and inflammatory bowel disease.
  39. PKM2 Kinase Inhibitor

    PKM2-IN-3 is a selective inhibitor of the PKM2 kinase, demonstrating an IC50 value of 4.1 μM. This compound exhibits notable anti-neuroinflammatory effects by disrupting PKM2-mediated glycolysis and inhibiting NLRP3 activation. PKM2-IN-3 is suitable for research applications focused on metabolic regulation and neuroinflammation pathways.
  40. AXL Inhibitor

    Denfivontinib hydrochloride is an AXL inhibitor that exerts synergistic antitumor effects when used in combination with the PD-1 inhibitor Pembrolizumab. This compound enhances the NOD-like receptor pathway, facilitating the formation of the NLRP3 inflammasome. Its unique mechanism of action makes it a valuable tool for cancer research, particularly in studying immune modulation and tumor progression.
  41. NF-κB Inhibitor

    NF-κB-IN-4 is a potent inhibitor of the NF-κB signaling pathway, demonstrating significant blood-brain barrier permeability. This compound exhibits anti-neuroinflammatory activity through its ability to block the phosphorylation and activation of IκBα, thereby reducing NLRP3 expression and inhibiting NF-κB activation. NF-κB-IN-4 is suitable for research applications related to neuroinflammatory diseases, providing a valuable tool for therapeutic investigations.

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