NLRP3
NLRP3 (NLR Family Pyrin Domain Containing 3) is a cytosolic pattern-recognition receptor that functions as the sensor component of the NLRP3 inflammasome, enabling innate immune cells to detect microbial motifs, endogenous danger signals, and environmental irritants[1]. Upon activation, NLRP3 oligomerizes and recruits the adaptor ASC and pro-caspase-1, leading to inflammasome assembly, caspase-1 activation, and subsequent maturation of the pro-inflammatory cytokines IL-1β and IL-18 as well as gasdermin D-mediated pyroptosis[1][2]. Mechanistically, canonical NLRP3 activation requires a priming step that enhances NLRP3 and pro-inflammatory cytokine expression, followed by an activation step triggered by diverse stimuli including extracellular ATP, microbial toxins, silica particles, and monosodium urate crystals[2]. Through these signaling processes, NLRP3 regulates inflammation, host defense, and immune homeostasis, while excessive activation promotes pathological inflammatory responses[1][3]. Dysregulated NLRP3 inflammasome activity has been implicated in autoinflammatory syndromes, gout, cardiovascular disease, neurodegenerative disorders, inflammatory bowel disease, and other inflammation-associated conditions[1][3][4]. Compared with other inflammasome-forming NOD-like receptors such as NLRP1 and NLRC4, NLRP3 is distinguished by its ability to respond to an exceptionally broad spectrum of pathogen-associated and danger-associated signals rather than a limited set of ligands[1][4]. For experimental applications, selective NLRP3 inhibitors such as MCC950 suppress inflammasome assembly by targeting the NACHT domain and are widely used to investigate NLRP3-dependent inflammatory mechanisms in preclinical disease models[4].
References:
- [1]. Swanson KV, et al. The NLRP3 inflammasome: molecular activation and regulation to therapeutics. Nat Rev Immunol. 2019 Aug;19(8):477-489. [Content Brief]
- [2]. Shin HJ, et al. Molecular mechanisms of NLRP3 inflammasome activation. Exp Mol Med. 2026 Mar;58(3):650-663. [Content Brief]
- [3]. Chen Y, et al. The NLRP3 inflammasome: contributions to inflammation-related diseases. Cell Mol Biol Lett. 2023 Jun 27;28(1):51. [Content Brief]
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NLRP3 Related Products (235)
Related Products (235)
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Recombinant Proteins (1)
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Antibodies (1)
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1,2,4-Trimethoxybenzene
0 ImagesCat. No.: HY-W017087CAS No.: 135-77-31,2,4-Trimethoxybenzene is an orally active NLRP3 selective inhibitor. 1,2,4-Trimethoxybenzene can markedly suppress Nigericin (HY-127019) or ATP (HY-B2176)-induced NLRP3 inflammasome activation, thus decreasing caspase-1 activation and IL-1β secretion. 1,2,4-Trimethoxybenzene specifically inhibits the activation of NLRP3 inflammasome without affecting absent in melanoma 2 (AIM2) inflammasome activation. 1,2,4-Trimethoxybenzene inhibits oligomerization of the apoptosis-associated speck-like protein containing a CARD (ASC) and protein-protein interaction between NLRP3 and ASC, thus blocking NLRP3 inflammasome assembly. 1,2,4-Trimethoxybenzene can be used for the study of experimental autoimmune encephalomyelitis (EAE), multiple sclerosis, and type 2 diabetes.
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Ro 106-9920
0 ImagesCat. No.: HY-107665CAS No.: 62645-28-7Ro 106-9920 is an orally active NF-κB inhibitor. Ro 106-9920 prevents ubiquitination of IκBα, blocks nuclear translocation of NF-κB, and inhibits NF-κB activation. Ro 106-9920 suppresses TNF-α-induced tissue factor expression and procoagulant activity, enhances TNF-α-mediated cytotoxicity against cancer cells, and eliminates the formation of neutrophil extracellular traps. Ro 106-9920 inhibits NLRP3 inflammasome activation, reduces inflammatory cytokine secretion, decreases myeloperoxidase activity, attenuates renal cell apoptosis, and improves renal function. Ro 106-9920 blocks ANG II (Angiotensin II human) (HY-13948)-induced nuclear localization of p65, internalization of AT1A receptor, colocalization of β-arrestin-2, and expression of COX-2, and alters the formation of β-arrestin endosomes. Ro 106-9920 can be used in research related to non-small cell lung cancer, acute kidney injury, diabetes mellitus, and osteoporosis.
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NT-0527
0 ImagesNT-0527 is a selective, orally active, and brain-permeable NLRP3 inflammasome inhibitor. NT-0527 can specifically block the formation of the NLRP3 inflammasome, resulting in the reduction in the maturation and release of IL-1β, exhibit inhibition on CYP2C19. NT-0527 displays anti-inflammatory activity in the mouse LPS (HY-D1056) /ATP (HY-B2176)-induced peritonitis model. NT-0527 can be used for the research of neuroinflammatory disorders (Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis) and peripheral inflammatory disorders (type II diabetes, atherosclerosis, gout, etc.) associated with NLRP3 inflammasome.
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(+)-Epiloliolide
0 ImagesCat. No.: HY-N10173CAS No.: 38274-00-9Synonyms: Isololiolide(+)-Epiloliolide is a megastigmane that can be isolated from Annona muricata. (+)-epiloliolide increased the nuclear localization of p53. (+)-Epiloliolide has anti-inflammatory effect through upregulating phosphorylation of the PKA/CREB pathway. (+)-Epiloliolide also effectively increases the proliferation and migration of human periodontal ligament cells by downregulating NLRP3 activated by PG-LPS.
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Isoandrographolide
0 ImagesIsoandrographolide is an orally active NLRP3 inflammasome inhibitor and AKT/GSK-3β/β-catenin pathway inhibitor. Isoandrographolide inhibits the expression of NLRP3, ASC, and caspase-1, and reduces the levels of phosphorylated AKT, phosphorylated GSK-3β, and β-catenin. Isoandrographolide alleviates inflammatory responses, reduces collagen deposition, suppresses epithelial-mesenchymal transition (EMT), induces differentiation of leukemia cells, inhibits the growth of leukemia cells, protects lung and kidney tissues, regulates cytokine levels, and also exhibits hepatoprotective effects. Isoandrographolide can be used in studies related to silicosis, murine myeloid leukemia, renal tubulointerstitial fibrosis, and non-alcoholic fatty liver disease.
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Benzylurea
0 ImagesBenzylurea is an anti-inflammatory agent. Benzylurea inhibits LPS (HY-D1056)-induced upregulation of MTCH2 expression and regulates pathways associated with mitochondrial function, inflammation and cell survival. Benzylurea alleviates LPS-induced proliferation inhibition and apoptosis of periodontal ligament fibroblasts, as well as the release of proinflammatory cytokines. Benzylurea can be used in studies related to periodontitis.
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NLRP3-IN-42
0 ImagesCat. No.: HY-163744CAS No.: 3040024-62-9
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NLRP3-IN-83
0 ImagesCat. No.: HY-175814NLRP3-IN-83 is a selective and orally active NLRP3 inflammasome activation inhibitor. NLRP3-IN-83 exhibits good inhibitory IL-1β activity with an IC50 of 1.4 μM by blocking NLRP3, independent of NF-κB signaling. NLRP3-IN-83 only slightly inhibits AIM2 inflammasome pathway, but has no effect on NLRC4 inflammasome. NLRP3-IN-83 prevent cell pyroptosis and exhibits significant anti-inflammatory efficacy in ulcerative colitis model. NLRP3-IN-83 can be used for the study of inflammatory bowel disease (IBD).
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NLRP3-IN-92
0 ImagesCat. No.: HY-184357CAS No.: 2557366-30-8NLRP3-IN-92 is a NLRP3 inflammasome inhibitor. NLRP3-IN-92 can be used for the research of immune diseases and inflammatory diseases.
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7-Oxogedunin
0 ImagesCat. No.: HY-178898CAS No.: 13072-74-77-Oxogedunin (Compound 7DG; Compound 16) is a small molecule that protects macrophages from cell pyroptosis induced by anthrax lethal toxin (LT). Its target is protein kinase R (PKR). 7-Oxogedunin can widely inhibit the assembly of various inflammasomes (NLRP1 and NLRP3) and the activation of caspase-1 by inhibiting the kinase-independent function of PKR. 7-Oxogedunin has growth inhibitory activity on European corn borer larvae. 7-Oxogedunin can be used for LT toxicity inhibition and pest control research.
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PRDX1-IN-4
0 ImagesCat. No.: HY-182287PRDX1-IN-4 is a PRDX1 inhibitor with an IC50 of 122 nM against human targets and high subtype selectivity. PRDX1-IN-4 covalently binds to PRDX1 to promote ROS accumulation. PRDX1-IN-4 inhibits NLRP3 inflammasome activation, blocks hepatic stellate cell activation and reduces collagen deposition. PRDX1-IN-4 induces apoptosis in activated hepatic stellate cells. PRDX1-IN-4 has good safety profile, with no significant body weight loss or hepatotoxicity observed in mice at a dose of 20 mg/kg. PRDX1-IN-4 ameliorates CCl4-induced liver injury and liver fibrosis in mice at a dose of 1 mg/kg. PRDX1-IN-4 can be used for the research of liver fibrosis.
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NLRP3-IN-70
0 ImagesCat. No.: HY-172134CAS No.: 1997362-01-2NLRP3-IN-70 (Compound 5m) is an NLRP3 inflammasome inhibitor with low oral bioavailability. NLRP3-IN-70 can directly bind to the NACHT domain of the NLRP3 protein and block the interaction of NLRP3 and ASC, thus inhibiting ASC oligomerization and NLRP3 inflammasome assembly. NLRP3-IN-70 can be used in the research of sepsis and nonalcoholic steatohepatitis.
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BLT1-IN-1
0 ImagesCat. No.: HY-181809BLT1-IN-1 is an orally active and selective BLT1 inhibitor with an IC50 of 8.7 nM and a Kd of 121 nM. BLT1-IN-1 exerts protective effects against acute lung injury and sepsis in in vivo models. BLT1-IN-1 can be used in research related to acute lung injury and sepsis.
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GFAP/NF-κB/APOE/NLRP3-IN-1
0 ImagesCat. No.: HY-183796GFAP/NF-κB/APOE/NLRP3-IN-1 is an orally active, blood-brain barrier-permeable multi-target inhibitor with an IC50 of 3.50 nM against Acetylcholinesterase. GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits BACE-1 with an IC50 of 14.61 nM. GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits Aβ1-42 aggregation with an IC50 of 8.63 μM. GFAP/NF-κB/APOE/NLRP3-IN-1 reduces the levels of GFAP, NLRP3 inflammasome, NF-κB and APOE. GFAP/NF-κB/APOE/NLRP3-IN-1 is applicable for the research of Alzheimer's disease and neuroblastoma.
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Yadanzigan
0 ImagesCat. No.: HY-N10312CAS No.: 76588-87-9Synonyms: YDZGYadanzigan (YDZG) is an anti-inflammatory agent and a NLRP3 inhibitor. Yadanzigan specifically inhibits NLRP3 activation via inhibiting NF-κB pathway and Reactive Oxygen Species production. Yadanzigan also moderates LPS (HY-D1056)-induced acute lung injury (ALI) in mice.
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NEK7 degrader-3
0 ImagesCat. No.: HY-185311CAS No.: 3119435-52-5NEK7 degrader-3 is an orally active and brain-penetrant NEK7 molecular glue degrader with a DC50 of 33.1 nM. NEK7 degrader-3 mediates interaction between NEK7 and E3 ligase cereblon, promoting proteasomal degradation of NEK7 and attenuating NLRP3 inflammasome-mediated inflammatory responses. NEK7 degrader-3 inhibits caspase-1 activity, cytokine release of IL-1β, IL-1α, and IL-18, and pyroptosis-related plasma membrane permeabilization. NEK7 degrader-3 shows antiinflammatory activity in an LPS (HY-D1056)-induced neuroinflammation mouse model. NEK7 degrader-3 can be used for the research of neuroinflammation.
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NLRP3-IN-9
0 ImagesCat. No.: HY-146802CAS No.: 2768759-64-2
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CXCR2-IN-3
0 ImagesCat. No.: HY-179387CXCR2-IN-3 is a CXCR2 inhibitor with an IC50 of 11.37 μM. CXCR2-IN-3 mediates CXCR2-Ca2+ signalling inhibition halted autophagic flux, subsequently facilitating ROS-mediated apoptotic cell death. CXCR2-IN-3 suppresses the CXCR2-NLRP3 canonical pathway, suppressing pre-tumorigenic markers. CXCR2-IN-3 causes autophagy-dependent cell death in polyploid giant cancer cells (PGCCs). CXCR2-IN-3 can be used for the research of oral squamous cell carcinoma (OSCC).
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JNUTS013
0 ImagesCat. No.: HY-182779CAS No.: 2763983-45-3JNUTS013 is a NLRP3 inflammasome inhibitor. JNUTS013 promotes proteasome-dependent degradation of NLRP3 and inhibits the release of downstream cytokines. JNUTS013 downregulates the expression of inflammation-related proteins including iNOS and COX-2. JNUTS013 exhibits anti-inflammatory activity and can be used in the research of inflammatory diseases.
