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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Anemoside A3-methyl 6-aminohexanoate
0 ImagesAnemoside A3-methyl 6-aminohexanoate is an orally effective pyruvate carboxylase (PC) inhibitor with a Kd value of 10.1 μM against human PC. Anemoside A3-methyl 6-aminohexanoate exerts its function through the PC/NF-κB/NLRP3 inflammasome axis. Anemoside A3-methyl 6-aminohexanoate significantly alleviates symptoms of DSS (HY-116282C)-induced colitis in mice. Anemoside A3-methyl 6-aminohexanoate can be used in colitis-related research.
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5-(3',4'-Dihydroxyphenyl)-γ-valerolactone
0 Images5-(3',4'-Dihydroxyphenyl)-γ-valerolactone is an intestinal microbiota metabolite of (-)-Epicatechin (HY-N0001). 5-(3',4'-Dihydroxyphenyl)-γ-valerolactone downregulates TNF-α-stimulated phosphorylation of IKK and IκBα, inhibits the transcriptional activation of NF-κB, and suppresses the expression of adhesion molecules and chemokines. 5-(3',4'-Dihydroxyphenyl)-γ-valerolactone promotes autophagy, alleviates oxidative stress, maintains osteoblast differentiation, induces G1 phase arrest, inhibits adipogenesis, and scavenges ABTS free radicals. 5-(3',4'-Dihydroxyphenyl)-γ-valerolactone inhibits the adhesion of uropathogenic Escherichia coli to bladder epithelial cells; when used in combination with Curcumin (HY-N0005), it downregulates the NLRP3 and NOX2/Nrf2 signaling pathways, thereby reducing microglial activation. 5-(3',4'-Dihydroxyphenyl)-γ-valerolactone can be used in research related to diabetes, atherosclerosis, osteoporosis, obesity, neurodegenerative diseases involving microglial activation, and urinary tract infections.
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Kanglexin
0 ImagesKanglexin is an orally active and novel anthraquinone compound. Kanglexin inhibits NLRP3 inflammatory body activation and cell pyroptosis, and has a cardioprotective effect. Kanglexin promotes angiogenesis through FGFR1/ERK signaling pathway and accelerates diabetic wound healing. In addition, Kanglexin has the effect of lipid-lowering and inhibiting the dedifferentiation of vascular smooth muscle cells, and can be used in the study of hyperlipidemia, fatty liver and atherosclerosis.
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BAL-1516
0 ImagesCat. No.: HY-175278BAL-1516 is an orally active NLRP3 inhibitor with human NLRP3 Kd of 14.2 nM, mouse NLRP3 Kd of 200 nM, and blood-brain barrier penetration.BAL-1516 binds to a surface groove of the NLRP3 nucleotide-binding domain, contacts FISNA and WHD subdomains, forms three hydrogen bonds to the peripheral β-strand of the triple-ATPase, and does not alter NLRP3 ATP-hydrolysis activity.BAL-1516 shows specificity for NLRP3 over other NOD-like receptors, directly binds mouse NLRP3, and inhibits inflammasome formation in monocytes and microglia.
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NLRP3-IN-2
0 ImagesNLRP3-IN-2, an intermediate substrate in the synthesis of glyburide, inhibits the formation of the NLRP3 inflammasome in cardiomyocytes and limits the infarct size following myocardial ischemia/reperfusion in the mouse, without affecting glucose metabolism.
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NLRP3-IN-79
0 ImagesNLRP3-IN-79 is an orally active NLRP3 inhibitor. NLRP3-IN-79 inhibits NLRP3 inflammasome with an IC50 of 10.69 nM. NLRP3-IN-79 blocks NLRP3 inflammasome assembly by directly binding to NLRP3 and disrupting the NEK7-NLRP3 interaction. NLRP3-IN-79 can be used for the study of NLRP3-driven diseases model, including systemic inflammation, peritonitis, and colitis.
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Antcin A
0 ImagesAntcin A is an orally active modulator of p53 and glucocorticoid receptor (GR), with an IC50 of 8.55 μM against human GR. Through transcriptional activation of p53, Antcin A induces miR-200c and inhibits ZEB1, regulates epithelial-mesenchymal transition markers, and suppresses cancer cell migration/invasion. Antcin A activates GR, inhibits Na+/K+-ATPase and NLRP3 inflammasome assembly, pyroptosis (pyroptosis) and pro-inflammatory cytokine release, reduces hepatic lipid deposition, improves liver function, and reverses metabolic changes induced by the SARS-CoV-2 spike protein. Antcin A can be used in research related to breast cancer, head and neck cancer, non-alcoholic fatty liver disease, and coronavirus disease 2019 (COVID-19).
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JC-171
0 ImagesJC-171 is a selective NLRP3 inflammasome inhibitor, with an IC50 of 8.45 μM for inhibiting LPS/ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages.
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ATP-15N5,d14 dilithium
0 ImagesCat. No.: HY-B2176S3Purity: 98%Synonyms: Adenosine 5'-triphosphate-15N5,d14 dilithiumATP-15N5,d14 (Adenosine 5'-triphosphate-ATP-15N5,d14) dilithium is the 15N5,d14-labeled ATP (HY-B2176). ATP is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation. ATP can activate the NLRP3 inflammasome and induce IL-1β and chemokines secretion. ATP has anti-bacterial infection effects and can protect mice against bacterial infection in mice.
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JT001
0 ImagesCat. No.: HY-156034CAS No.: 2238819-65-1Synonyms: NLRP3-IN-19JT001 (NLRP3-IN-19) is a potent, specific and orally active inhibitor of NLRP3. JT001 can inhibit NLRP3 inflammasome assembly, resulting in the inhibition of cytokine release and the prevention of pyroptosis. JT001 can be used for the research of nonalcoholic steatohepatitis and liver fibrosis.
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PROTAC HDAC6 degrader 7
0 ImagesCat. No.: HY-179421CAS No.: 3133307-16-8PROTAC HDAC6 degrader 7 is an orally active, highly efficient, and selective PROTAC degrader targeting histone deacetylase 6 (HDAC6) (IC50 = 118 nM). PROTAC HDAC6 degrader 7 can eliminate both the catalytic and zinc-finger ubiquitin-binding domain. PROTAC HDAC6 degrader 7 inhibits NLRP3 inflammasome assembly and activation, as well as blocks NF-κB signaling, thereby reducing the transcription and release of key inflammatory factors. PROTAC HDAC6 degrader 7 can reduce the mRNA levels of NLRP3, pro-IL-1β, TNF-α, and IL-6. PROTAC HDAC6 degrader 7 can be used for the study of inflammatory bowel disease (IBD).
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RP-220
0 ImagesCat. No.: HY-P6084CAS No.: 1541177-35-8RP-220 is a renalase peptide targeting NLRP3. RP220 has anti-inflammatory and anti-apoptotic activities. RP220 inhibits renal tubular epithelial cells apoptosis with alkaline insult by activating MAPK signaling pathway. RP220 significantly inhibits NLRP3 expression and reduces macrophage infiltration and kidney tissue damage in acute kidney injury (AKI) mice model. RP-220 can be uses for systemic lupus erythematosus (SLE) and its complication lupus nephritis (LN) research.
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MC-ND-18
0 ImagesCat. No.: HY-162588CAS No.: 3081572-53-1MC-ND-18 is an ATTEC degrader that degrades NLRP3 via the Autophagy pathway, with a DC50 of 125.5 nM in THP-1 cells. MC-ND-18 exhibits anti-inflammatory activity in a DSS-induced mouse model of colitis. MC-ND-18 can be used for research on inflammatory bowel disease. MC-ND-18 consists of an NLRP3 inhibitor (HY-156121), a linker (HY-W018745), and an LC3 ligand.
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NLRP3-IN-11
0 ImagesNLRP3-IN-11 is a NLR family pyrin domain containing 3 (NLRP3) proteins inhibitor. NLRP3-IN-11 has biological activity for NLRP3 with an IC50 value of <0.3 μM. NLRP3-IN-11 can be used for the researh of inflammatory and degenerative diseases including NASH, atherosclerosis and other cardiovascular diseases, Alzheimer's disease, Parkinson's disease, diabetes, gout, and numerous other autoinflammatory diseases.
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NP3-146 sodium
0 ImagesNP3-146 sodium is a NLRP3 inflammasome inhibitor through locking the NACHT domain of NLRP3. NP3-146 sodium shows potent inhibitory activity against IL-1β release with an IC50 value of 0.171 μM in LPS (HY-D1056)/Nigericin (HY-127019)-stimulated BMDM cells. NP3-146 sodium regulates the levels of cleaved Caspase-1 and cleaved IL-1β in cell supernatants. NP3-146 sodium can be used for the research of inflammatory diseases.
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Impanoflast Sodium
0 ImagesCat. No.: HY-161297CAS No.: 2763617-39-4Synonyms: NT-0249NT-0249 is an orally active NLRP3 inhibitor. NT-0249 has anti-inflammatory activity
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NLRP3-IN-NBC6
0 ImagesCat. No.: HY-131040CAS No.: 2068818-02-8NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor (IC50= 574 nM) that acts independently of Ca2+. NLRP3-IN-NBC6 inhibits Nigericin (HY-127019)-induced inflammasome activation in THP-1 cells and Imiquimod (HY-B0180)-induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs).
