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Inhibitors | Molecular mechanism | Cell/animal model/patients | Ref |
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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] |
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