NLRP3 Inflammasome and Inflammatory Diseases

Table 2

Inhibitors of NLRP3 pathways as well as their effects in cell cultures, animal models, or patients of inflammatory diseases.

Inhibitors	Molecular mechanism	Cell/animal model/patients	Ref
MCC950	Block the ATPase domain of NLRP3 and inhibit the activation of typical and atypical NLRP3 inflammasome	Autoimmune encephalomyelitis; Cryopyrin-associated periodic syndrome; Muckle-Wells syndrome	[124]
MNS	Bind to the LRR and NACHT domains and suppress ATPase activity of NLRP3	Bone marrow-derived macrophages	[91]
CY-09	Inhibit NLRP3 ATPase activity	Cryopyrin-associated autoinflammatory syndrome; Type 2 diabetes; Synovial fluid cells from gout patients	[137]
OLT1177	Inhibit NLRP3 ATPase activity and block canonical and noncanonical activation of NLRP3 inflammasome	Human blood-derived macrophages; Human blood neutrophils; Monocytes isolated from patients with cryopyrin-associated periodic syndrome; Spleen cells from mice	[128]
Glyburide	Inhibit ATP-sensitive K^+ channels, act as downstream of the P2X7 receptor, and inhibit ASC aggregation	Bone marrow-derived macrophages; Familial cold-associated autoinflammatory syndrome patients	[129]
16673-34-0	Interfere the downstream of NLRP3 conformational changes and bind to ASC	Acute myocardial infarction	[138]
JC124	Block ASC aggregation, caspase-1 activation, and IL-1β secretion	Acute myocardial infarction; Alzheimer’s disease	[139]; [140]
BHB	Inhibit K^+ efflux and block ASC aggregation	Muckle-Wells syndrome; Familial cold autoinflammatory syndrome; Urate crystal-induced peritonitis	[70]
Parthenolide	Inhibit caspase-1 activation and NLRP3 ATPase activity	Bone marrow-derived macrophages; Cystic fibrosis	[131]; [141]
Bay 11-7082	Alkylation of cysteine residues of the NLRP3 ATPase region	Psoriasis-like dermatitis; Diabetic nephropathy	[142]; [143]