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. 2020 Jun 11;21(11):4184. doi: 10.3390/ijms21114184

Table 1.

NLRP3 inflammasome deactivators.

Inhibitor Target and Mechanism Refs
GKT137831 Inhibits NOX4 activity and reduces fatty acid oxidation pathway [135]
VAS-2870 Inhibits NOX4 activity and reduces fatty acid oxidation pathway [135]
Etomoxir Inhibits CPT1A, a key enzyme in fatty acid oxidation pathway [135]
C75 & cerulenin Inhibits FASN activity that reduces the phosphorylation of AKT and p38 MAPK [136]
CY-09 Impairs ATPase activity of NLRP3 via binding to its ATP binding site in NACHT domain [137]
MNS Impairs ATPase activity of NLRP3 via cysteine modification [138]
OLT1177 Impairs ATPase activity of NLRP3 [139]
BOT-4-one Impairs ATPase activity of NLRP3 [140]
INF39 Impairs ATPase activity of NLRP3 via binding to its ATP binding site in NACHT domain [141]
Parthenolide Impairs ATPase activity of NLRP3; Suppresses IκB kinase and NF-κB [142,143,144]
Bay 11-7082 Impairs ATPase activity of NLRP3; Suppresses IκB kinase and NF-κB [142]
Tranilast Interferes with NLRPP3–NLRP3 and NLRP3–ASC interaction [145]
Oridonin Interferes with NLPR3–NEK7 interaction [139]
Metformin Activates AMPK that reduces ER stress and mitochondrial fission [146]
Resveratrol Activates AMPK that reduces ER stress and mitochondrial fission [146]
Glycyrrhizin Blocks TLR4 that reduces downstream NF-κB and p38 MAPK activation; Inhibits kinase activity of IKK; Inhibits ASC oligomerization via unknown mechanism [147]
Isoliquiritigenin Blocks TLR4 that reduces downstream NF-κB and MAPK activation; Inhibits transcriptional activity of NF-κB; Inhibits ASC oligomerization via unknown mechanism [147]
Berberine Enhances AMPK-dependent autophagy that eliminates mtROS; [148]
Melatonin Reduces protein abundance of NF-κB and p65 [149]
Eplerenone Inhibits phosphorylation of NF-κB and ROS production [150]
β-hydroxybutyrate Abolishes K+ efflux; Reduces ASC oligomerization and speck formation via unknown mechanism [151]
IL-10 Inhibits mTOR and promote mitophagy [152]