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].
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].
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].
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).
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].
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].
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].
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.
Dapansutrile (OLT1177) is a potent, selective and orally active inhibitor of NLRP3 inflammasome. Anti-inflammatory, analgesic activity[1].
iE-DAP is a biological active peptide. (NOD1 agonist)
ADS032 is a dual inhibitor of NLRP1 and NLRP3 that can rapidly, reversibly and stably inhibit inflammasome formation. ADS032 can reduce NLPR1 and NLRP3 activation of human macrophages and bronchial epithelial cells to secrete and mature IL-1β and TNF-α, and reduce NLRP3-induced ASC speck formation. ADS032 protected mice against the deadly influenza A virus, reducing inflammation in the lungs and improving survival. ADS032 inhibits Nigericin (HY-127019)-induced IL-1β secretion with IC50s of 94.6 μM (No wash out) and 354 μM (Wash out) respectively[1].
TriDAP (L-Ala-γ-D-Glu-meso-diaminopimelic acid) is a biological active peptide. (specific Nod1 activator)
NT-0796 is a selective and CNS-penetrant NLRP3 inflammasome inhibitor with an IC50 of 0.32 nM in PBMC assay. NT-0796 is an isopropyl ester that undergoes intracellular conversion to NDT-19795, the carboxylic acid active species. NT-0796 has the potential for neuroinflammatory diseases research[1].
CP-424174 is a reversible inhibitor against IL-1β processing with an IC50 of 210 nM.CP-424174 indirectly inhibits NLRP3[1].
C12-iE-DAP (Lauroyl-γ-D-glutamyl-meso-diaminopimelic acid) is a biological active peptide. (a lauroyl (C12) group to the glutamic residue of iE-DAP , NOD1 agonist)
NLRP3 modulators 1 is the potent modulator of NLRP3. NLRP3 modulators 1 agonizes or partially agonizes NLRP3 that are useful for researching a condition, disease or disorder in which a decrease in LRP3 activity contributes to the pathology (extracted from patent WO2017184746A1, compound 107)[1].
NLRP3-IN-25 (compound 32) is an orally available NLRP3 inhibitor with anti-inflammatory activity. NLRP3-IN-25 attenuates renal injury in doxorubicin-induced glomerulonephritis in mice. NLRP3-IN-25 inhibits IL-1β secretion in THP-1 cells with an IC50 of 21 nM[1].
MR2938 is a potent AChE inhibitor, with an IC50 of 5.04 μM. MR2938 also suppresses NO production obviously (IC50 = 3.29 μM). MR2938 suppresses the neuroinflammation through blocking MAPK/JNK and NF-κB signaling pathways. MR2938 can be used for Alzheimer’s disease (AD) research[1].
NLRP3-IN-15 is a potent and selective NLRP3 inflammasome inhibitor. NLRP3-IN-15 inhibits IL-1β release with an IC50 of 0.114 μM. NLRP3-IN-15 can be used for the research of inflammation[1].
M-TriDAP (N-Acetylmuramyl-L-Ala-γ-D-Glu-meso-diaminopimelic acid) is a biological active peptide. (NOD1/2 Agoist)
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.
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].
Selnoflast (example 6) is a NLRP3 inhibitor (extracted from patent WO2019008025)[1].