Muscone is the main active monomer of traditional Chinese medicine musk. Muscone inhibits NF-κB and NLRP3 inflammasome activation. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6), and ultimately improves cardiac function and survival rate[1].
M-TriDAP (N-Acetylmuramyl-L-Ala-γ-D-Glu-meso-diaminopimelic acid) is a biological active peptide. (NOD1/2 Agoist)
NIC-0102 is an orally active proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammatory vesicle activation. NIC-0102 shows potent anti-inflammatory effects in a model of dextran sulfate sodium (DSS)-induced ulcerative colitis. NIC-0102 also inhibits production of pro-IL-1β[1].
JT001 (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[1].
D359-0396 is an orally active NLRP3 inflammasome inhibitor. D359-0396 inhibits pyroptosis and IL-1β release in macrophages. D359-0396 also inhibits the oligomerization of NLRP3, ASC and the cleavage of GSDMD. D359-0396 alleviates EAE, and also improves survival after septic shock in mice[1].
Nodinitib-1 (ML130;CID-1088438) is a NOD1 inhibitor with an IC50 of 0.56 μM.
NLRP3-IN-5 is a NLRP3 inflammasome inhibitor (WO2016131098 (N-((4-chloro-2,6-dimethylphenyl)carbamoyl)-4-(2-hydroxypropan-2- l)furan-2-sulfonamide))[1].
Articaine (Hoe-045 free base) is an amide anaesthetic containing an ester group, reversibly binding to the α-subunit of the voltage-gated sodium channels within the inner cavity of the nerve, can provide effective pain relief. Articaine ameliorates LPS-induced acute kidney injury via inhibition of NF-ĸB activation and the NLRP3 inflammasome pathway[1][2][3].
GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells[1].
JC-171 is a selective NLRP3 inflammasome inhibitor that inhibits LPS/ATP-induced IL-1β release from macrophages with IC50 of 8.45 uM; interferes with NLRP3/ASC interaction induced by LPS/ATP stimulation both in vtiro and in vivo; delays the progression and reduces the severity of experimental autoimmune encephalomyelitis (EAE).
Selnoflast (example 6) is a NLRP3 inhibitor (extracted from patent WO2019008025)[1].
NLRP3-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[1].
NLRP3-IN-10 is a potent NLRP3 inhibitor, inhibits IL-1β release with an IC50 value of 251.1 nM. NLRP3-IN-10 suppresses NLRP3 inflammasome activation by attenuating ASC speck formation[1].
NOD2 antagonist 1 (compound 32) is a potent and selective NOD2 antagonist with an IC50 of 5.23 μM. NOD2 antagonist 1 inhibits Muramyl dipeptide (MDP)-induced IL-8 secretion in THP-1 cells and inhibits MDP-induced IL-6, IL-10, TNF-α release in PBMCs[1].
NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-bindingoligomerization domain-like receptor 1/2) dual antagonist, with IC50 values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX)[1].
MCC950 sodium is a potent, selective NLRP3 inhibitor with IC50s of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively.
INF4E is a potent NLRP3 inflammasome inhibitor. INF4E inhibits caspase-1 and NLRP3 ATPase activities. INF4E shows protection against the IR-induced myocardial injury and dysfunction[1][2].
Usnoflast is a NLRP3 modulator, as well as a non-steroidal anti-inflammatory agent (NSAD)[1].
NLRP3 antagonist 1 is a potent antagonist of NLRP3. NLRP3 is mainly expressed in macrophages and neutrophils and is involved in the body's intrinsic immunity against pathogenic infections and stress injury. NLRP3 antagonist 1 has the potential for the research of cancer disease (extracted from patent WO2021114691A1, compound 3)[1].
JC124 is a specific NLRP3 inflammasome inhibitor. JC124 has anti-inflammatory and neuroprotective effects[1].
NLRP3-IN-21 (compound L38) is a NLRP3 inflammasome inhibitor with inflammatory properties. NLRP3-IN-21 inhibits NLRP3 inflammasome activation and pyroptosis by suppressing gasdermin D cleavage, ASC oligomerization, and NLRP3 inflammasome assembly[1].
Troxerutin, also known as vitamin P4, is a tri-hydroxyethylated derivative of natural bioflavonoid rutins which can inhibit the production of reactive oxygen species (ROS) and depress ER stress-mediated NOD activation.
NLRP3-IN-20 (compound 11) is an orally available inhibitor of the NLRP3 inflammasome with an IC50 of 25 nM for IL-1β secretion. NLRP3-IN-20 has excellent pharmacokinetic properties and demonstrated significant efficacy in models of non-alcoholic steatohepatitis, fatal septic shock, and colitis[1].
NLRP3-IN-9 is a potent NLRP3 inhibitor. NLRP3-IN-9 inhibits IL-1β release. NLRP3-IN-9 reduces inflammation and mechanical hyperalgesia. NLRP3-IN-9 has the potential for the research of gout[1].
BMS-986299 (compound 112) is a first-in-class NLRP3 inflammasome agonist with an EC50 of 1.28 μM. (patent WO2018152396A1).
seco-Isolariciresinol Diglucoside, a synthetic lignin, which is derived from the natural plant flaxseed. seco-Isolariciresinol Diglucoside reduces asbestos-induced NLRP3 expression, and NF-κB activation in macrophages (MF). seco-Isolariciresinol Diglucoside also activates Nrf2.
Fc 11a-2, a benzimidazole compound, is an orally active and potent NLRP3 inflammasome inhibitor. Fc 11a-2 restrains the formation of NLRP3 inflammasome by inhibiting activation of caspase-1 and thus the activation of IL-1b/IL-18. Fc 11a-2 prevents the development of Dextran sulfate sodium (DSS; HY-116282C)-induced murine experimental colitis[1][2][3].
Soyasaponin II is a saponin with antiviral activity. Soyasaponin II inhibits the replication of HSV-1, HCMV, influenza virus, and HIV-1. Soyasaponin II shows potent inhibition on HSV-1 replication. Soyasaponin II serves as a inhibitor for YB-1 phosphorylation and NLRP3 inflammasome priming and could protect mice against LPS/GalN induced acute liver failure[1][2].
NLRP3 agonist 1 (compound 23) is a potent and orally active NLRP3 agonist. NLRP3 agonist 1 can activate the enzyme Caspase-1 to cleave pro-IL-1β and pro-IL-18 proinflammatory cytokines into their mature forms[1].
Dapansutrile (OLT1177) is a potent, selective and orally active inhibitor of NLRP3 inflammasome. Anti-inflammatory, analgesic activity[1].