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. 2020 Mar 12;8:140. doi: 10.3389/fcell.2020.00140

TABLE 1.

Inhibitors against NLRP3 inflammasome.

Target specificity Inhibitor Diseases Clinical status References
NLRP3 MCC950 Inflammatory diseases Phase II Coll et al., 2015
NLRP3 Tranilast (MK-341) Inflammatory diseases Approved Huang et al., 2018
NLRP3 OLT1177 Inflammatory diseases Phase II Marchetti et al., 2018
NLRP3 CY-09 Inflammatory diseases Preclinical Jiang et al., 2017
NLRP3 JC171 Inflammatory diseases Preclinical Guo et al., 2017
NLRP3 JC124 Traumatic neuroinflammatory response Preclinical Kuwar et al., 2019
NLRP3 INF39 Inflammatory diseases Preclinical Cocco et al., 2017
NLRP3 NBCs Inflammatory diseases Preclinical Baldwin et al., 2017
NLRP3 Apigenin Inflammatory diseases Preclinical Lim et al., 2018
NLRP1, NLRP3, NK-κB, IKKβ Parthenolide Inflammatory diseases, Cystic fibrosis Preclinical Juliana et al., 2010
NLRP3 ILG Obesity, hypercholesterolemia, and insulin resistance Preclinical Honda et al., 2014
NLRP3 Fc11a-2 Inflammatory diseases Preclinical Liu et al., 2013
NLRP3 NLRP3 BOT-4-one Inflammatory diseases Preclinical Shim et al., 2017
NLRP3 Glyburide Inflammatory diseases Preclinical Lamkanfi et al., 2009
NLRP3 MNS Inflammatory diseases Preclinical He et al., 2014
NLRP3 Flufenamic acid Alzheimer’s disease Preclinical Daniels et al., 2016
NLRP3 16673-34-0 Acute myocardial infarction Preclinical Marchetti et al., 2014
NLRP3 Oridonin Inflammatory diseases Preclinical He et al., 2018
NLRP3 Kynurenic acid Stress-related colonic disorder Preclinical Zheng et al., 2019
NLRP3 Formononetin Inflammatory diseases Preclinical Wu D. et al., 2018
NLRP3 Triptolide Cardioprotective Preclinical Li et al., 2017
NLRP3 Andrographolide Inflammatory diseases Preclinical Guo et al., 2014
NLRP3 Celastrol Inflammatory diseases Preclinical Xin et al., 2017
NLRP3 BHB Inflammatory diseases Preclinical Youm et al., 2015
Caspase-1 Caspase-1 VX-740 Inflammatory diseases Preclinical Rudolphi et al., 2003
Caspase-1 VX-765 Inflammatory diseases Preclinical Wannamaker et al., 2007
IL-1R1 Anakinra Cystic fibrosis Approved Iannitti et al., 2016
IL-1β Canakinumab Cardiovascular events Approved Shah et al., 2018
IL-1β Gevokizumab Cardiac remodeling and coronary dysfunction Preclinical Harouki et al., 2017
IL-1β Pralnacasan Inflammatory diseases Preclinical Rudolphi et al., 2003
Cytokines IL-1β Curcumin Inflammatory diseases Preclinical Gong et al., 2018
IL-1βR Rilonacept CAPS Approved Gillespie et al., 2010
IL-1α Xilonix Femoral artery restenosis Phase II El Sayed et al., 2016
IL-4/IL-13 SAR156597 IPF Phase II Raghu et al., 2018
TGF-β SHP-627 Cardiac fibrosis Preclinical Zhang et al., 2012
PDGFR Imatinib NSF, IPF Phase II Daniels et al., 2010
Endothelin-1 receptor Macitentan Heart failure Phase II NCT03153111
Angiotensin II Losartan Cardiac fibrosis Preclinical Gay-Jordi et al., 2013
Related pathways Relaxin receptor Serelaxin Cardiac fibrosis Preclinical Wu X. P. et al., 2018
IKK IMD-1041 Cardiac fibrosis Preclinical Tanaka et al., 2012
IKK Bardoxolone methyl Pulmonary hypertension Phase II Chin et al., 2018
NF-κB BAY 11-7082 Inflammatory diseases Preclinical Irrera et al., 2017
NK-κB Baicalein Renal fibrosis Preclinical Zhao et al., 2016
NF-κB Wogonoside Inflammatory diseases Preclinical Sun et al., 2015
JNK Tanzisertib (CC930) IPF Phase II NCT01203943
TLR-4 Alpinetin Inflammatory diseases Preclinical He X. et al., 2016
MAPK MMI-0100 Cardiac fibrosis Preclinical Meng et al., 2017
Peroxiredoxin 1 AI-44 Inflammatory diseases Preclinical Liu W. et al., 2018
AhR/Nrf2/NQO1 Cardamonin Inflammatory diseases Preclinical Wang K. et al., 2018
AMPK/ULK1/p62 Ginsenoside Rd Inflammatory diseases Preclinical Liu C. et al., 2018
Cathepsin B VBY-376 Liver fibrosis Preclinical Wree et al., 2016
Smad2/4 Pentoxifylline Cardiac fibrosis Preclinical Zhang et al., 2016
NOX4 GKT-137831 Cardiac fibrosis Preclinical Zhao et al., 2015
ROS N-acetylcysteine Cardiac fibrosis Preclinical Giam et al., 2016
ROS Levornidazole Inflammatory diseases Preclinical Wang et al., 2015
ROS Mitoquinone Cardiac fibrosis Preclinical Goh et al., 2019
ROS LGM2605 Radiation damage Preclinical Chatterjee et al., 2019