nlrp3 inflammasome

NLRP3-IN-2 (5-Chloro-N-(p-sulfamoylphenethyl)-o-anisamide), an intermediate capable of synthesizing glibenclamide, exerts an inhibitory effect on the formation of NLRP3 inflammatory vesicles in cardiomyocytes, limiting infarct size after myocardial ischemia/reperfusion in mice and has no effect on metabolism.

NLRP3 AIM2-IN-3 is a unique molecule that inhibits NLRP3 and AIM2 inflammasome activation in a species-specific manner. It has an IC50 value for cell lysis of 0.077 ± 0.008 μ M. NLRP3 AIM2-IN-3 is a potent inhibitor of NLRP3 and AIM2 inflammasome-dependent cell lysis with an IC50 value for cell lysis of 0.077 ± 0.008 μ M. NLRP3 AIM2-IN-3 inhibits LPS nigericin NLRP3 AIM2-IN-3 inhibits LPS nigericin-stimulated cell lysis in THP-1 macrophages with an IC50 value of 0.077 ± 0.008 μM. NLRP3 AIM2-IN-3 interferes with the interaction of NLRP3 or AIM2 with the bridging protein ASC, inhibiting oligomerization of ASC.

Nigericin sodium salt is an antibiotic, an NLRP3 activator, and a cationic ion carrier. Nigericin sodium triggers the activation of the NALP3 inflammasome, which inhibits Golgi function and suppresses the growth of Gram-positive bacteria.

Muscone (3-Methylcyclopentadecanone) is an organic compound that is the primary contributor to the odor of musk.

ATP disodium salt (Adenosine-Triphosphate) is a P2 purinoceptor agonist.

ATP disodium salt hydrate (Adenosine disodium triphosphate) is a nucleoside triphosphate used in cells as a coenzyme often called the molecular unit of currency of intracellular energy transfer.

ATP (Adenosine triphosphate) provides cellular energy, participates in overall energy balance, and maintains intracellular homeostasis. ATP can act as an extracellular signaling molecule through interactions with specific purinergic receptors to mediate a variety of processes including neurotransmission, inflammation, apoptosis, and bone remodeling.

Lobeglitazone Sulfate（CKD-501 Sulfate） is a novel thiazolidinedione with anti-inflammatory activity that inhibits LPS-induced NLRP3 inflammasome activation and hepatic inflammation, and can be used in the study of type 2 diabetes mellitus (T2DM).

NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor with an IC50 of 574 nM. It acts independently of Ca 2+ and inhibits Nigericin-induced inflammasome activation in THP-1 cells, as well as Imiquimod-induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs) [1].

NT-0796 is a brain-permeable, potent, and selective inhibitor of the inflammasome NLRP3, inhibiting NLRP3 activation.NT-0796 is a potential NDT-19795 delivery vector.

Dapansutrile is a potent, selective and orally active NLRP3 inflammasome inhibitor, with Anti-inflammatory and analgesic activity.

CP-456773 (MCC950 (CP-456773) and CRID3) is an effective and specific cytokine release inhibitor and NLRP3 inflammasome inhibitor. CP-456773 inhibits IL-1β secretion and caspase 1 processing. MCC950 blocked canonical and noncanonical NLRP3 activation at nanomolar concentrations. MCC950 specifically inhibited activation of NLRP3 but not the AIM2, NLRC4 or NLRP1 inflammasomes. MCC950 reduced IL-1β production in vivo and attenuated the severity of experimental autoimmune encephalomyelitis (EAE), a disease model of multiple sclerosis.

CP 424174 is an inhibitor of IL-1β post-translational processing with IC50 of 210 nM. Inhibits the formation of mature IL-1β. Indirectly inhibits NLRP3. Active in vivo and orally bioavailable.

NLRP3-IN-9 (INF-4E) is an inhibitor of NLRP3 ATPase and caspase-1. NLRP3-IN-9 acts by irreversibly trapping thiol nucleophiles, which prevents both ATP- and nigericin-triggered pyroptosis of human THP-1 cells in a time- and concentration-dependent manner.

YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 µM and exhibits significant anti-inflammatory activity.

4'-Methoxyresveratrol (4'-O-Methylresveratrol) is a natural product from the roots of *Rheum palmatum* L., with significant hypoglycemic, anti-inflammatory, and antioxidant effects. 4'-Methoxyresveratrol alleviates AGE-induced inflammation by suppressing RAGE-mediated MAPK NF-κB signaling pathway and NLRP3 inflammasome activation.

hydrocotarnine is an inhibitor of Cbl.

Stavudine sodium (d4T), an orally active nucleoside reverse transcriptase inhibitor (NRTI), demonstrates activity against both HIV-1 and HIV-2. It also inhibits mitochondrial DNA (mtDNA) replication, reduces NLRP3 inflammasome activation, modulates Amyloid-β autophagy, and induces apoptosis [1] [2] [3] [4].

NLRP3-IN-4 is a highly efficient and orally bioavailable inhibitor of NLRP3 inflammasome, which exhibits strong anti-inflammatory properties specifically targeted towards colitis.

NLRP3-IN-16 is a potent, selective inhibitor of the NLRP3 inflammasome, effectively reducing IL-1β release with an IC50 of 0.065 μM, and is primarily utilized in inflammation research [1].

NLRP3-IN-17 is a potent, selective, and orally active inhibitor of the NLRP3 inflammasome with an IC50 of 7 nM, effectively inhibiting NLRP3-dependent IL-1β secretion in mice, making it valuable for chronic inflammatory disease research [1].

NLRP3-IN-21 (compound L38) is an inhibitor of the NLRP3 inflammasome with anti-inflammatory properties, suppressing inflammasome activation and pyroptosis by inhibiting gasdermin D cleavage, ASC oligomerization, and NLRP3 inflammasome assembly [1].

Isoandrographolide, a compound known for its cell differentiation-inducing and hepatoprotective effects, also inhibits NLRP3 inflammasome activation and mitigates silicosis in mice.

GDC-2394, an orally active, selective NLRP3 inhibitor, also targets IL-1β, exhibiting inhibitory concentrations (IC50s) of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β). It effectively hampers NLRP3-induced caspase-1 activity while not affecting NLRC4-dependent inflammasome activation.

NLRP3-IN-15 is a potent, selective inhibitor of the NLRP3 inflammasome, demonstrating efficacy by inhibiting IL-1β (interleukin-1 beta) release with an IC50 value of 0.114 μM. This compound is utilized in the research of inflammation.

Articaine (Hoe-045 free base), an amide anesthetic featuring an ester group, effectively relieves pain by reversibly binding to the α-subunit of the voltage-gated sodium channels located in the nerve's inner cavity. Furthermore, Articaine mitigates LPS-induced acute kidney injury through the suppression of NF-κB activation and inhibition of the NLRP3 inflammasome pathway.

Hexokinase (ScHEX1), a glycolytic enzyme, is inhibited by n-acetylglucosamine, which causes it to detach from the mitochondrial outer membrane. This detachment activates the NLRP3 inflammasome [1].

JC-171, a selective inhibitor of the NLRP3 inflammasome, effectively inhibits LPS ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages with an IC50 of 8.45 μM[1].

Peptide5 TFA, a connexin 43 mimetic peptide, mitigates swelling, astrogliosis, and neuronal cell death in animal models of spinal cord injury, and suppresses the NLRP3 inflammasome, functioning as an anti-inflammatory agent (1) (2) (3).

QS-21, an immunostimulatory saponin, is a potent vaccine adjuvant that stimulates both Th2 humoral and Th1 cell-mediated immune responses by interacting with antigen presenting cells (APCs) and T cells. Furthermore, QS-21 activates the NLRP3 inflammasome, leading to the release of cytokines IL-1β and IL-18, dependent on caspase-1.

NLRP3-IN-14 is a potent, selective inhibitor of the NLRP3 inflammasome, displaying a dissociation constant (K D) of 5.87 μM and an IC50 of 0.131 μM for inhibiting IL-1β release. It is applicable for inflammation research.

Emlenoflast (MCC7840) is a selective inhibitor of NLRP3 inflammasome.

Emlenoflast sodium (MCC7840 sodium), a sulfonylurea, is a selective NLRP3 inflammasome inhibitor with an IC50 value of less than 100 nM for NLRP3 inflammasome, and can be used in the study of inflammatory diseases.

JT002 is an orally active NLRP3 inflammasome inhibitor that decreases the production of NLRP3-dependent proinflammatory cytokines (such as IL-1β, IL-1α, IL-18) and pyroptosis, as well as inhibits the formation of the NLRP3 inflammasome complex. Additionally, JT002 mitigates airway hyperresponsiveness and airway neutrophilia in mice [1].

JT001 (NLRP3-IN-19) is a potent, specific, and orally active NLRP3 inhibitor that impedes the assembly of the NLRP3 inflammasome, suppressing cytokine release and preventing pyroptosis. JT001 is utilized in research on nonalcoholic steatohepatitis and liver fibrosis [1].

Azalamellarin N is a pyroptosis inhibitor that exhibits varying inhibitory effects on different pyroptosis inducers. It functions by targeting molecules upstream of NLRP3 inflammasome activation, instead of directly affecting the components of the NLRP3 inflammasome. Its inhibitory potency against various inducers is ranked as follows: Nigericin > R837 [1].

NLRP3-IN-10 (ZVN26391) is a potent NLRP3 inhibitor. NLRP3-IN-10 inhibits IL-1β release with an IC50 value of 251.1 nM. NLRP3-IN-10 attenuates ASC speck formation, leading to suppress activation of NLRP3 inflammasome.

A 68930 is a dopamine D-1 receptor antagonist. A 68930 inhibits NLRP3 inflammasome activity.

NLRP3-IN-12 is a specific inhibitor of the NLRP3 inflammasome that targets the NLRP3 protein to effectively reduce IL-1β release, with an IC50 of 0.45 μM. This compound is utilized in the research of inflammatory bowel disease (IBD).

Oxidized ATP trisodium salt (oATP) is a broad-spectrum P2 receptor inhibitor that irreversibly antagonizes P2X7R activation and inhibits CRP-induced NLRP3 inflammasome activation, making it useful in atherosclerosis research [1] [2].

NLRP3-IN-23 (Compound 15C) is an inhibitor that significantly impedes heme-mediated activation of the NLRP3 inflammasome at a concentration of 0.1 μM [1].

NLRP3-IN-7 (Compound 36) is a selective inhibitor of the NLRP3 inflammasome and can assemble the NLRP3 inflammasome.

NP3-146 (NLRP3-IN-5) is an inflammasome NLRP3 inhibitor with potential anti-inflammatory activity for the study of autoimmune diseases.

NLRP3-IN-38 (Compound 18) serves as an inhibitor of the NOD-like receptor protein 3 (NLRP3), effectively blocking the activation of the NLRP3 inflammasome with an EC50 value of 23 nM [1].

NDT-19795 is a potent NLRP3 inflammasome inhibitor with an IC 50 value of 66 nM using the PBMC method and 4.7 μM using the WB method. It is a carboxylic acid-active compound that can be derived from NT-0796 within cells, and is applicable for neurological disease research [1].

Anti-inflammatory agent 50 (compound a1), a derivative of Fusidic acid, exerts its effects through inhibition of inflammatory mediators including NO, IL-6, and TNF-α. It mitigates acute lung injury by modulating these mediators and suppressing the MAPK, NF-κB, and NLRP3 inflammasome signaling pathways [1].

NPBA, a potassium K2P channel TASK-3 (KCNK9) agonist, concurrently functions as a blocker of the tandem pore domain weak inward rectifying K+ channel (TWIK2). This compound effectively inhibits NLRP3 inflammasome activation in macrophages [1].

Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and no intrinsic sympathomimetic activity.

NLRP3-IN-6 (Compound 34) is a selective NLRP3 inflammasome inhibitor.

Compound 14a (P2X7 receptor antagonist-4) is a P2X7R antagonist with IC50 values of 64.7 nM in humans and 10.1 nM in mice. It inhibits the activation of the NLRP3 inflammasome, which subsequently reduces the expression of caspase-1, gasdermin D, IL-1β, and IL-18 in the kidneys of mice with sepsis-induced damage [1].