S7809 |
MCC950 Sodium
|
MCC950 Sodium is a potent, selective inhibitor of NLRP3 with IC50 of 7.5 nM in BMDMs; but not the AIM2, NLRC4 or NLRP1 inflammasomes. |
-
Circ Res, 2024, 135(9):933-950
-
Bone Res, 2024, 12(1):53
-
Int J Biol Sci, 2024, 20(9):3393-3411
|
|
S8930 |
MCC950
|
MCC950 (CP-456773, CRID3) is a potent and selective inhibitor of NLRP3 (NOD-like receptor (NLR) family, pyrin domain-containing protein 3) with IC50 of 7.5 nM and 8.1 nM in BMDMs and HMDMs, respectively. |
-
Int J Biol Sci, 2024, 20(14):5695-5714
-
Cell Death Dis, 2024, 15(1):43
-
Cell Prolif, 2024, e13720.
|
|
S6653 |
Nigericin sodium salt
|
Nigericin sodium salt is an antibiotic derived from Streptomyces hygroscopicus that works by acting as an H+, K+, and Pb2+ ionophore.Nigericin can activate NLRP3 inflammasome to induce pro-inflammatory and immunostimulatory processes. |
-
Biomed Pharmacother, 2024, 174:116548
-
Biomed Pharmacother, 2024, 180:117512
-
J Anim Sci Biotechnol, 2024, 15(1):116
|
|
S5774 |
CY-09
|
CY-09 is a specific NLRP3 inflammasome inhibitor that directly targeted NLRP3 itself. It is tested against the five major cytochrome P450 enzymes 1A2, 2C9, 2C19, 2D6, and 3A4 with half maximal inhibitory concentration (IC50) values of 18.9, 8.18, >50, >50, and 26.0 µM, respectively. |
-
iScience, 2024, 27(3):109118
-
Antioxidants (Basel), 2023, 12(3)722
-
J Exp Clin Cancer Res, 2022, 41(1):74
|
|
S8559 |
INF39
|
INF39 is a nontoxic, irreversible NLRP3 inhibitor that counteracts NLRP3 activation through direct irreversible interaction with NLRP3 and partial inhibition of LPS-driven pro-inflammatory gene expression. |
-
Chin Med J (Engl), 2022, 135(12):1474-1485
-
Biomed Res Int, 2022, 2022:7250578
-
Int Immunopharmacol, 2021, 92:107358
|
|
S3680 |
NLRP3 Inflammasome Inhibitor I
|
NLRP3 Inflammasome Inhibitor I, an intermediate substrate in the synthesis of glyburide which is free of the cyclohexylurea moiety involved in insulin release, is a novel inhibitor of the NLRP3 inflammasome. |
-
eprints, 2023, 10.14943/doctoral.k15475
-
Am J Pathol, 2022, S0002-9440(22)00076-1
-
Immunopharmacol Immunotoxicol, 2022, 1-24
|
|
S8907 |
Dapansutrile
|
Dapansutrile is a novel and selective NLRP3 inflammasome inhibitor. |
-
iScience, 2023, 26(3):106089
-
iScience, 2023, 26(3):106089
|
|
S3871 |
Muscone
|
Muscone (3-Methylcyclopentadecanone, Methylexaltone), a flavouring ingredient, is an organic compound that is the primary contributor to the odor of musk and also a potent anti-inflammatory agent. Muscone significantly downregulats the levels of LPS-induced inflammatory cytokines and inhibits NF-κB and NLRP3 inflammasome activation in BMDMs. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6). |
-
J Pharm Pharmacol, 2019, 71(11):1706-1713
|
|
S3939 |
4'-Methoxyresveratrol
|
4-Methoxyresveratrol is a stibenoid found in the Chinese herb Gnetum cleistostachyum. 4'-Methoxyresveratrol alleviates AGE-induced inflammation through suppressing RAGE-mediated MAPK/NF-κB signaling pathway and NLRP3 inflammasome activation. |
|
|
E0138 |
YQ128
|
YQ128 is a selective inhibitor of NLRP3 with an IC50 of 0.30 µM.
|
|
|
S3290 |
Procyanidin B2 (PCB2)
|
Procyanidin B2 (PCB2), a natural flavonoid found in commonly consumed foods, possess anti-inflammatory, anti-oxidant and anti-cancer activities. Procyanidin B2 activates PPARγ to induce M2 polarization in mouse macrophages. Procyanidin B2 significantly suppresses the activation of NLRP3 inflammasome in the lung tissue induced by paraquat in the rat model. |
-
BMC Cardiovasc Disord, 2024, 24(1):231
-
Front Pharmacol, 2021, 12:639651
|
|
S9899 |
BMS-986299
|
BMS-986299 is a novel NLRP3 agonist that induces IL8 release to activate natural killer (NK) cells.
|
|
|
E1970New |
BAL-0028
|
BAL-0028 (Compound 3), which belongs to the indazole class is an inhibitor of NLRP3 activation with an IC50 value of 25 nM. BAL-0028 binds tightly to the NACHT domain of NLRP3, with KD values ranging from 104 to 123 nM. BAL-0028 also exhibits anti-inflammatory activity. |
|
|
E3652 |
Rehmanniae radix praeparata Extract
|
Rehmanniae radix praeparata Extract is extracted from Rehmanniae radix praeparata, which can improve diabetes through AMPK-mediated NF-κB/NLRP3 signaling pathway. |
|
|
E4663New |
INF195
|
INF 195 is an NLRP3 inhibitor which inhibits NLRP3-driven macrophage pyrodeath and IL-1β release. At low dose, INF 195 can reduce the infarct size of isolated mouse hearts and effectively prevent myocardial ischemia/reperfusion injury. |
|
|
E3367 |
Garlic chives Extract
|
Garlic chives Extract is extracted from Allium tuberosum, which provides a new therapeutic in the treatment of NLRP3 inflammasome-driven diseases. |
|
|
E1281 |
Dimethyl itaconate
|
Dimethyl itaconate can reprogram neurotoxic to neuroprotective primary astrocytes through the regulation of LPS-induced Nod-like receptor protein 3 (NLRP3) inflammasome and nuclear factor 2/heme oxygenase-1 (NRF2/HO-1) pathways. |
|
|
E1872New |
Selnoflast
|
Selnoflast(RO-7486967) is a selective and reversible small molecule inhibitor of NLRP3 inflammasome, with the potential to treat moderate to severe active ulcerative colitis. |
|
|
S9261 |
Shionone
|
Shionone is a triterpenoid component derived from the herbal medicine Aster tataricus, anit has anti-inflammatory properties. Shionone specifically inhibits NLRP3 inflammasome activation in vitro and in vivo.
|
-
J Cardiothorac Surg, 2024, 19(1):435
|
|
E0225 |
Licochalcone B
|
Licochalcone B (Lico B), extracted from Glycyrrhiza uralensis Fisch, induces the cell cycle arrest and apoptosis in human hepatoma cell HepG2. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7‐NLRP3 interaction.
|
|
|
S7809 |
MCC950 Sodium
|
MCC950 Sodium is a potent, selective inhibitor of NLRP3 with IC50 of 7.5 nM in BMDMs; but not the AIM2, NLRC4 or NLRP1 inflammasomes. |
- Circ Res, 2024, 135(9):933-950
- Bone Res, 2024, 12(1):53
- Int J Biol Sci, 2024, 20(9):3393-3411
|
|
S8930 |
MCC950
|
MCC950 (CP-456773, CRID3) is a potent and selective inhibitor of NLRP3 (NOD-like receptor (NLR) family, pyrin domain-containing protein 3) with IC50 of 7.5 nM and 8.1 nM in BMDMs and HMDMs, respectively. |
- Int J Biol Sci, 2024, 20(14):5695-5714
- Cell Death Dis, 2024, 15(1):43
- Cell Prolif, 2024, e13720.
|
|
S5774 |
CY-09
|
CY-09 is a specific NLRP3 inflammasome inhibitor that directly targeted NLRP3 itself. It is tested against the five major cytochrome P450 enzymes 1A2, 2C9, 2C19, 2D6, and 3A4 with half maximal inhibitory concentration (IC50) values of 18.9, 8.18, >50, >50, and 26.0 µM, respectively. |
- iScience, 2024, 27(3):109118
- Antioxidants (Basel), 2023, 12(3)722
- J Exp Clin Cancer Res, 2022, 41(1):74
|
|
S8559 |
INF39
|
INF39 is a nontoxic, irreversible NLRP3 inhibitor that counteracts NLRP3 activation through direct irreversible interaction with NLRP3 and partial inhibition of LPS-driven pro-inflammatory gene expression. |
- Chin Med J (Engl), 2022, 135(12):1474-1485
- Biomed Res Int, 2022, 2022:7250578
- Int Immunopharmacol, 2021, 92:107358
|
|
S3680 |
NLRP3 Inflammasome Inhibitor I
|
NLRP3 Inflammasome Inhibitor I, an intermediate substrate in the synthesis of glyburide which is free of the cyclohexylurea moiety involved in insulin release, is a novel inhibitor of the NLRP3 inflammasome. |
- eprints, 2023, 10.14943/doctoral.k15475
- Am J Pathol, 2022, S0002-9440(22)00076-1
- Immunopharmacol Immunotoxicol, 2022, 1-24
|
|
S8907 |
Dapansutrile
|
Dapansutrile is a novel and selective NLRP3 inflammasome inhibitor. |
- iScience, 2023, 26(3):106089
- iScience, 2023, 26(3):106089
|
|
S3871 |
Muscone
|
Muscone (3-Methylcyclopentadecanone, Methylexaltone), a flavouring ingredient, is an organic compound that is the primary contributor to the odor of musk and also a potent anti-inflammatory agent. Muscone significantly downregulats the levels of LPS-induced inflammatory cytokines and inhibits NF-κB and NLRP3 inflammasome activation in BMDMs. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6). |
- J Pharm Pharmacol, 2019, 71(11):1706-1713
|
|
S3939 |
4'-Methoxyresveratrol
|
4-Methoxyresveratrol is a stibenoid found in the Chinese herb Gnetum cleistostachyum. 4'-Methoxyresveratrol alleviates AGE-induced inflammation through suppressing RAGE-mediated MAPK/NF-κB signaling pathway and NLRP3 inflammasome activation. |
|
|
E0138 |
YQ128
|
YQ128 is a selective inhibitor of NLRP3 with an IC50 of 0.30 µM.
|
|
|
S3290 |
Procyanidin B2 (PCB2)
|
Procyanidin B2 (PCB2), a natural flavonoid found in commonly consumed foods, possess anti-inflammatory, anti-oxidant and anti-cancer activities. Procyanidin B2 activates PPARγ to induce M2 polarization in mouse macrophages. Procyanidin B2 significantly suppresses the activation of NLRP3 inflammasome in the lung tissue induced by paraquat in the rat model. |
- BMC Cardiovasc Disord, 2024, 24(1):231
- Front Pharmacol, 2021, 12:639651
|
|
E1970New |
BAL-0028
|
BAL-0028 (Compound 3), which belongs to the indazole class is an inhibitor of NLRP3 activation with an IC50 value of 25 nM. BAL-0028 binds tightly to the NACHT domain of NLRP3, with KD values ranging from 104 to 123 nM. BAL-0028 also exhibits anti-inflammatory activity. |
|
|
E3652 |
Rehmanniae radix praeparata Extract
|
Rehmanniae radix praeparata Extract is extracted from Rehmanniae radix praeparata, which can improve diabetes through AMPK-mediated NF-κB/NLRP3 signaling pathway. |
|
|
E4663New |
INF195
|
INF 195 is an NLRP3 inhibitor which inhibits NLRP3-driven macrophage pyrodeath and IL-1β release. At low dose, INF 195 can reduce the infarct size of isolated mouse hearts and effectively prevent myocardial ischemia/reperfusion injury. |
|
|
E3367 |
Garlic chives Extract
|
Garlic chives Extract is extracted from Allium tuberosum, which provides a new therapeutic in the treatment of NLRP3 inflammasome-driven diseases. |
|
|
E1872New |
Selnoflast
|
Selnoflast(RO-7486967) is a selective and reversible small molecule inhibitor of NLRP3 inflammasome, with the potential to treat moderate to severe active ulcerative colitis. |
|
|
S9261 |
Shionone
|
Shionone is a triterpenoid component derived from the herbal medicine Aster tataricus, anit has anti-inflammatory properties. Shionone specifically inhibits NLRP3 inflammasome activation in vitro and in vivo.
|
- J Cardiothorac Surg, 2024, 19(1):435
|
|
E0225 |
Licochalcone B
|
Licochalcone B (Lico B), extracted from Glycyrrhiza uralensis Fisch, induces the cell cycle arrest and apoptosis in human hepatoma cell HepG2. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7‐NLRP3 interaction.
|
|
|