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Immunology/Inflammation

Aryl Hydrocarbon Receptor

Immunology/Inflammation related

NOD-like Receptor (NLR)

Prostaglandin Receptor

Reactive Oxygen Species

Thrombopoietin Receptor

NOD-like Receptor (NLR)

The nucleotide-binding oligomerization domain-like receptors, or NOD-like receptors (NLRs) (also known as nucleotide-binding leucine-rich repeat receptors), are intracellular sensors of pathogen-associated molecular patterns (PAMPs) that enter the cell via phagocytosis or pores, and damage-associated molecular patterns (DAMPs) that are associated with cell stress. They are types of pattern recognition receptors (PRRs), and play key roles in the regulation of innate immune response. NLRs can cooperate with toll-like receptors (TLRs) and regulate inflammatory and apoptotic response. They are found in lymphocytes, macrophages, dendritic cells and also in non-immune cells, for example in epithelium. NLRs are highly conserved through evolution. Their homologs have been discovered in many different animal species (APAF1) and also in the plant kingdom (disease-resistance R protein).

Filter HomeSignaling PathwaysImmunology/InflammationNOD-like Receptor (NLR)

Nigericin sodium salt

T309228643-80-3

Nigericin sodium salt is an antibiotic, an NLRP3 activator, and a cationic ion carrier. Nigericin sodium triggers the activation of the NALP3 inflammasome, which inhibits Golgi function and suppresses the growth of Gram-positive bacteria.

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MCC950 sodium

T6887256373-96-3

MCC950 sodium (CP-456773 sodium) is a potent and selective inhibitor of the inflammatory vesicle NLRP3 (IC50=7.5 nM in BMDMs; IC50=8.1 nM in HMDMs). MCC950 sodium has no effect on other inflammatory vesicles such as AIM2, NLRC4 or NLRP1.

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NOD-IN-1

T3587132819-92-2

NOD-IN-1 (Compound 4) is a potent mixed inhibitor of nucleotide-binding oligomerization domain (NOD)-like receptors.

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Nodinitib-1

T6591799264-47-4

Nodinitib-1 (CID-1088438) is a potent and selective NOD1 inhibitor with an IC50 of 0.56 μM.

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CY-09

T41641073612-91-5

CY-09 is an NLRP3 inhibitor.

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Dapansutrile

T1505254863-37-5

Dapansutrile is a potent, selective and orally active NLRP3 inflammasome inhibitor, with Anti-inflammatory and analgesic activity.

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Troxerutin

T07727085-55-4

Troxerutin (Trihydroxyethylrutin), a natural bioflavonoid, is isolated from Sophora japonica. It has many benefits and medicinal properties.

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Ruscogenin

T6S1256472-11-7

1. Ruscogenin has anti-inflammatory activity, suppressed zymosan A-evoked peritoneal total leukocyte migration in mice in a dose-dependent manner, 2. Ruscogenin inhibited adhesion of leukocytes to a human umbilical vein endothelial cell line (ECV34) injured by tumor necrosis factor-alpha (TNF-alpha) in a concentration-dependent manner. 3. Ruscogenin significantly attenuate LPS-induced acute lung injury via inhibiting expressions of TF and iNOS and NF-kappa B p65 activation.

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JC2-11

T77579937820-89-8

JC2-11 is an inhibitory compound for inflammation.JC2-11 inhibits the recruitment domain-containing proteins NLRC 4, atypical in melanoma 2 (AIM 2) and atypical (NC) inflammatory vesicles by disrupting reactive oxygen species (ROS) production and caspase-1 activity.JC2-11 reduces caspase-1 (p20) secretion, gasdermin D (GSDMD) cleavage, IL-1β and lactate dehydrogenase (LDH) activity in inflammatory vesicles. JC2-11 reduced caspase-1 (p20) secretion, gasdermin D (GSDMD) cleavage, IL-1β and lactate dehydrogenase (LDH) release from inflammatory vesicles.

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YQ128

T133752454246-18-3

YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 µM and exhibits significant anti-inflammatory activity.

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Muscone

T2893541-91-3

Muscone (3-Methylcyclopentadecanone) is an organic compound that is the primary contributor to the odor of musk.

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Arglabin

TQ016584692-91-1

Arglabin ((+)-Arglabin) is a natural product isolated from Artemisia glabella, is a NLRP3 inflammasome inhibitor, has anti-atherogenic and anticancer effects.

$106

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INF39

T4217866028-26-4

INF39 is a noncytotoxic and irreversible NLRP3 inhibitor.

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Trimethylamine N-oxide

T412451184-78-7

Trimethylamine N-oxide (TMAO) is a colorless amine oxide produced from choline, betaine, and carnitine via intestinal microbial metabolism that accumulates in tissues of marine animals and prevents the protein-damaging effects of urea.Trimethylamine N-oxide induces inflammation through activation of ROS NLRP3 inflammasomes, which can induce fibroblast differentiation and cardiac fibrosis.

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Magnesium isoglycyrrhizinate hydrate

TN7831658701-67-8

Magnesium isoglycyrrhizinate hydrate (18α-Glycyrrhizic acid Magnesium hydrate) is an active ingredient derived from licorice with anti-inflammatory properties. It lowers alanine and aspartate aminotransferase activities and can be used in HIV-1 infection research.

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CORM-3

T6454475473-26-8

CORM-3 is a carbon monoxide-releasing molecule with anti-inflammatory and cardioprotective activity.

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Stavudine

T14043056-17-5

Stavudine (BMY-27857), a nucleoside reverse transcriptase inhibitor analog of thymidine, has activity against HIV.

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NLRP3-IN-2

T323016673-34-0

NLRP3-IN-2 (5-Chloro-N-(p-sulfamoylphenethyl)-o-anisamide), an intermediate capable of synthesizing glibenclamide, exerts an inhibitory effect on the formation of NLRP3 inflammatory vesicles in cardiomyocytes, limiting infarct size after myocardial ischemia reperfusion in mice and has no effect on metabolism.

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Emlenoflast

T92221995067-59-8

Emlenoflast (MCC7840) is a selective inhibitor of NLRP3 inflammasome.

$116

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NLRP3-IN-67

T2032523055022-81-3

NLRP3-IN-67 (compound 42) is an effective inhibitor of NLRP3.

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10-14 weeks

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NLRP3-IN-63

T2031673064696-02-9

NLRP3-IN-63 (Compound 7) is an inhibitor of NLRP3, effectively suppressing NLRP3 activation with an EC50 of 13 nM.

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10-14 weeks

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NLRP3-IN-21

T788942956791-61-8

NLRP3-IN-21 (compound L38) is an inhibitor of the NLRP3 inflammasome with anti-inflammatory properties, suppressing inflammasome activation and pyroptosis by inhibiting gasdermin D cleavage, ASC oligomerization, and NLRP3 inflammasome assembly [1].

$1,520

8-10 weeks

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NLRP3-IN-16

T730152906872-59-9

NLRP3-IN-16 is a potent, selective inhibitor of the NLRP3 inflammasome, effectively reducing IL-1β release with an IC50 of 0.065 μM, and is primarily utilized in inflammation research [1].

$1,520

6-8 weeks

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NLRP3-IN-17

T781682254432-75-0

NLRP3-IN-17 is a potent, selective, and orally active inhibitor of the NLRP3 inflammasome with an IC50 of 7 nM, effectively inhibiting NLRP3-dependent IL-1β secretion in mice, making it valuable for chronic inflammatory disease research [1].

$140

5 days

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INF200

T79446

INF200 (compound 5), a sulfonylurea-based inhibitor of NLRP3 and associated pyroptosis, exhibits cardiometabolic benefits in a rat model of high-fat diet (HFD)-induced metaflammation and demonstrates anti-inflammatory effects by reducing IL-1β release in human macrophages at a concentration of 10 μM. Additionally, it enhances glucose and lipid profiles, diminishes systemic inflammation and cardiac dysfunction biomarkers, notably BNP, and ameliorates myocardial damage linked to ischemia reperfusion injury (IRI) as assessed by hemodynamic parameters [1].

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TriDAP

T80267877462-71-0

TriDAP (L-Ala-γ-D-Glu-meso-diaminopimelic acid), a biologically active peptide, functions as a specific Nod1 activator.

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Oxidized low density lipoprotein (Human)

T200276

Oxidized low density lipoprotein (Human) (Human ox-LDL) plays a crucial role in atherogenesis and contributes to endothelial dysfunction through the cytoplasmic adapter protein TRAF3IP2. This compound also promotes endothelial cell activation, leads to increased production of adhesion molecules, and reduces eNOS activity and NO production. Additionally, Human ox-LDL activates the NLRP3 inflammasome in macrophages.

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NLRP3-IN-49

T200567

NLRP3-IN-49 (compound Z48) is a potent and specific inhibitor of NLRP3, displaying IC50 values of 0.26 μM in THP-1 cells and 0.21 μM in mouse bone marrow-derived macrophages. It directly binds to the NLRP3 protein with a dissociation constant (Kd) of 1.05 μM, effectively preventing the assembly and activation of the NLRP3 inflammasome, thereby exhibiting anti-inflammatory properties. NLRP3-IN-49 is utilized in the research of inflammatory bowel disease.

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NLRP3-IN-46

T200610

NLRP3-IN-46 (Compound 3k) activates the cholinergic anti-inflammatory pathway involved in neuro-immune modulation, thereby inhibiting the activation of the NLRP3 inflammasome. Furthermore, NLRP3-IN-46 suppresses the production of IL-1β in THP-1 cells induced by Uric acid sodium, making it relevant for research in gouty arthritis.

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NOD1-IN-1

T200671687627-78-7

NOD1 2-IN-1 (Compound 2) is a potent inhibitor of RIPK2 with an IC50 value of 0.65 nM as determined by the ADP-Glo assay. It selectively inhibits the NOD1 pathway, with an IC50 of 33 nM, effectively blocking the production of pro-inflammatory cytokines and thereby reducing inflammatory responses. This compound has potential applications in the research of colitis.

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10-14 weeks

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Neral

T201808106-26-3

Neral, a monoterpenoid compound, exhibits anti-inflammatory and anticancer activities. It inhibits TNF-α and IL-6, along with inflammatory mediators such as pro-IL-1β, iNOS, COX-2, and NLRP-3.

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10-14 weeks

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NLRP3-IN-64

T2036573047549-19-6

NLRP3-IN-64 (Compound 2) is an inhibitor of NLRP3, effectively suppressing its activation with an EC50 of 5 nM.

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10-14 weeks

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JT002

T788222238820-43-2

JT002 is an orally active NLRP3 inflammasome inhibitor that decreases the production of NLRP3-dependent proinflammatory cytokines (such as IL-1β, IL-1α, IL-18) and pyroptosis, as well as inhibits the formation of the NLRP3 inflammasome complex. Additionally, JT002 mitigates airway hyperresponsiveness and airway neutrophilia in mice [1].

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8-10 weeks

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Selnoflast potassium

T78614

Selnoflast (potassium) (example 6), is an NLRP3 inhibitor.

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NLRP3-IN-19

T796952238819-65-1

JT001 (NLRP3-IN-19) is a potent, specific, and orally active NLRP3 inhibitor that impedes the assembly of the NLRP3 inflammasome, suppressing cytokine release and preventing pyroptosis. JT001 is utilized in research on nonalcoholic steatohepatitis and liver fibrosis [1].

$1,520

6-8 weeks

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NLRP3-IN-44

T899533040298-34-5

NLRP3-IN-44 (compound P33), an orally active (approximately 62%) and potent inhibitor of NLRP3, exhibits a dissociation constant (K D) of 17.5 nM. This compound is crucial in the research of diseases mediated by the NLRP3 inflammasome.

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10-14 weeks

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NLRP3-IN-58

T2009692956014-05-2

NLRP3-IN-58 (Compound DS15) acts as an inhibitor of NLRP3 inflammasome activation, with an IC50 value of 3.85 μM, and is capable of inhibiting 33% of IL-1β release at a concentration of 10 μM.

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10-14 weeks

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NOD2 agonist 3

T200865

NOD2agonist 3 (Compound 5) is an effective NOD2 agonist with an EC50 value of 111.45 nM, demonstrating immunoenhancing properties.

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NOD1/2-IN-1

T200582

NOD1 2-IN-1 (Compound 18) is a potent RIPK2 inhibitor, demonstrating an IC50 value of 1.4 nM in the ADP-Glo assay. It blocks the production of pro-inflammatory cytokines by inhibiting the NOD1 NOD2 pathway (IC50 values are 18 nM and 170 nM for NOD1 and NOD2, respectively), thereby reducing inflammatory responses. This compound is utilized in research related to colitis.

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AChE/BChE-IN-23

T201792

AChE BChE-IN-23 (Compound 6e) is a dual inhibitor of acetylcholinesterase and butyrylcholinesterase, exhibiting IC50 values of 0.91 μM for AChE, 1.19 μM for eqBChE, and 1.01 μM for hBChE. This compound also demonstrates antioxidant properties and inhibits the aggregation of Aβ1-42 and Tau proteins. Moreover, AChE BChE-IN-23 prevents the activation of microglial cells by inhibiting the release of reactive oxygen species and mitochondrial damage. Additionally, it reduces the levels of the NLRP3 inflammasome in human microglial cells and reverses memory impairment in mice induced by scopolamine.

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10-14 weeks

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NLRP3-IN-66

T2030203052155-88-8

NLRP3-IN-66 (example 257) is a potent inhibitor of the NLRP3 inflammasome.

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10-14 weeks

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Anti-neuroinflammation agent 1

T79590

Anti-neuroinflammation Agent 1 effectively modulates BV2 microglia cell polarization, shifting from an M1 to an M2 phenotype [1].

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Selnoflast calcium

T786132887416-19-3

Selnoflast calcium (example 6), an NLRP3 inhibitor[1], is a chemical compound designed to suppress the activity of the NLRP3 inflammasome.

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NLRP3-IN-20

T797332428478-22-0

NLRP3-IN-20 (compound 11) is an orally administered inhibitor targeting the NLRP3 inflammasome, exhibiting potent inhibition with an IC50 of 25 nM against IL-1β secretion. It possesses excellent pharmacokinetic properties and has shown significant efficacy in models of non-alcoholic steatohepatitis, fatal septic shock, and colitis [1].

$1,520

6-8 weeks

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D359-0396

T826211031977-31-7

D359-0396, an orally active NLRP3 inflammasome inhibitor, mitigates pyroptosis and reduces IL-1β release in macrophages by inhibiting the oligomerization of NLRP3, ASC, and the cleavage of GSDMD. The compound is effective in alleviating Experimental Autoimmune Encephalomyelitis (EAE) and enhances survival following septic shock in mice [1].

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8-10 weeks

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NLRP3-IN-55

T201017

NLRP3-IN-55 (Compound 19) is an effective inhibitor of NLRP3, exhibiting an inhibitory concentration (IC50) of 0.34 μM. It targets the NLRP3 protein directly with a dissociation constant (KD) of 0.45 μM, effectively blocking the assembly and activation of the NLRP3 inflammasome. This action results in anti-inflammatory effects and inhibits cell pyroptosis.

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NLRP3-IN-57

T201467

NLRP3-IN-57 (compound 5) inhibits the NLRP3 inflammasome, consequently downregulating IL-1β levels in THP-1 macrophages induced by LPS+Nigericin.

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10-14 weeks

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NOD1-RIPK2-IN-1

T201625

NOD1-RIPK2-IN-1 (Compound 37) is an inhibitor of the NOD1-RIPK2 signaling pathway, displaying potent IC50 values of 42 nM and 1.52 nM against NOD1 and RIPK2, respectively. This compound effectively reduces the secretion of the pro-inflammatory cytokine IL-8, making it valuable for research in inflammation and immune disorders.

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