Table 2.
Inhibitors of NLRP3 inflammasome.
| Inhibitor | Structure | Mechanism of action | Inhibition of priming | Refs |
|---|---|---|---|---|
| Glyburide |
|
N/A | N/A | (119–122) |
| MCC950 |
|
Binds to walker B motif of NATCH domain to inhibit ATPase activity and close active conformation | No | (123–126) |
| Flufenamic acid (Fenamate) |
|
Reversible blockade of Cl channel volume-regulated anion channels (VRAC) | N/A | (127) |
| CY-09 |
|
Binds to the Walker A motif of NLRP3 to impair the ATP binding of NLRP3 and suppresses its ATPase activity | No | (128) |
| Tranilast |
|
Binds to the NACHT domain of NLRP3 to block NLRP3 oligomerization | Yes | (129) |
| MNS |
|
Binds with NACHT and LRR domain and inhibit ATPase | Yes | (130) |
| Bay11-7082 |
|
Inhibits ATPase activity of NLRP3 | Yes | (131) |
| OLT1177 |
|
Prevents NLRP3-ASC and NLRP3-caspase-1 interaction, inhibits ATPase activity of NLRP3 | No | (132) |
| BHB |
|
Prevents K+ efflux | N/A | (133) |
| INF39 |
|
Irreversibly interacts with NLRP3 and affects NLRP3 conformational change that could be related with the ATPase activity | Yes | (134) |
| BOT-4-one |
|
NLRP3 alkylation, impairs ATPase activity of NLRP3, enhances the ubiquitination level of NLRP3 | Yes | (135) |
| Oridonin |
|
Covalently bond with the cysteine 279 of NLRP3 in NACHT domain to inhibit NLRP3-NEK7 interaction | No | (136) |
| Licochalcone B |
|
Binds to NEK7 and disrupts NEK7-NLRP3 interaction | Yes | (137) |
| Echinatin |
|
Binds to HSP90, blocks its ATPase activity and abolishes the association between the cochaperone SGT1 and HSP90-NLRP3 | N/A | (138) |
| Curcumin |
|
Prevents K+ efflux, inhibits microtubule-driven recruitment of ASC on mitochondrion to NLRP3 on the endoplasmic reticulum | Yes | (139) |
| Cardamonin |
|
N/A | No | (140) |
| Carnosol |
|
Binds to HSP90 and inhibits HSP90 activity | Yes | (141) |
| Cryptotanshinone |
|
Suppresses Ca2+ signaling and mitochondrial reactive oxygen species (mtROS) induction | No | (142) |
N/A, Not Applicable.