NOD

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.

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.

Bergenin (Bengenin) is a polyphenol, which is an effective antinarcotic agent with antioxidant action.

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.

Lobeglitazone Sulfate（CKD-501 Sulfate） is a novel thiazolidinedione with anti-inflammatory activity that inhibits LPS-induced NLRP3 inflammasome activation and hepatic inflammation, and can be used in the study of type 2 diabetes mellitus (T2DM).

antcin A is a steroid-like phytochemical isolated from the fruiting bodies of a precious edible mushroom Antrodia cinnamomea with strong anti-inflammatory and anti-tumor effects.

Selnoflast (example 6) is a NLRP3 inhibitor[1].

ADS032 (BT-032) is an NLRP1 and NLRP3 inhibitor with anti-inflammatory activity,, inhibits the activation of NLRP1 and NLRP3, inhibits Nigericin-induced IL-1β production, and can be used to study respiratory inflammation or infection.

Muramyl dipeptide (MDP) is a synthetic immunoreactive peptide, consisting of N-acetyl muramic acid attached to a short amino acid chain of L-Ala-D-isoGln. Muramyl dipeptide indirectly decreases osteoclast differentiation through a decreased RANKL/OPG ratio. Muramyl dipeptide directly increases osteoblast differentiation by up-regulating Runx2 gene expression through MAPK pathways. Muramyl dipeptide is an inducer of bone formation through the induction of Runx2 .

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

CP-456773 (MCC950 (CP-456773) and CRID3) is an effective and specific cytokine release inhibitor and NLRP3 inflammasome inhibitor. CP-456773 inhibits IL-1β secretion and caspase 1 processing. MCC950 blocked canonical and noncanonical NLRP3 activation at nanomolar concentrations. MCC950 specifically inhibited activation of NLRP3 but not the AIM2, NLRC4 or NLRP1 inflammasomes. MCC950 reduced IL-1β production in vivo and attenuated the severity of experimental autoimmune encephalomyelitis (EAE), a disease model of multiple sclerosis.

Molsidomine (Corvaton) is an orally active, long-acting vasodilating drug. It metabolizes in the liver to the active metabolite linsidomine, that releases nitric oxide (NO) upon decay as the actual vasodilating compound.

NLRP3-IN-11 is an NLRP3 protein inhibitor with potential anti-inflammatory activity.NLRP3-IN-11 can be used in the study of atherosclerosis and parkinsonism.

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

L-Canavanine sulfate is a selective inducible NO synthase inhibitor.

NLRP3-IN-10 (ZVN26391) is a potent NLRP3 inhibitor. NLRP3-IN-10 inhibits IL-1β release with an IC50 value of 251.1 nM. NLRP3-IN-10 attenuates ASC speck formation, leading to suppress activation of NLRP3 inflammasome.

Emlenoflast sodium (MCC7840 sodium), a sulfonylurea, is a selective NLRP3 inflammasome inhibitor with an IC50 value of less than 100 nM for NLRP3 inflammasome, and can be used in the study of inflammatory diseases.

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

BMS986299 is a modulator of NLRP3 with an EC50 of 1.28 μM and can be used in studies about NLRP3 signaling and the treatment of associated diseases.

6-Biopterin (L-Biopterin) is a natural product,is a NO synthase cofactor.

7,4'-Dihydroxyflavone (4',7-Dihydroxyflavone) can induce transcription of nodulation (nod) genes in Rhizobium meliloti. It has inhibitory activities against COX-2.

JC124 is an inhibitor of NLRP3 Inflammasome and exhibits neuroprotective and anti-inflammatory activities.

Imperatorin (8-Isopentenyloxypsoralene) is a modulator of p38, ERK pathway. Imperatorin increases BMP-2 expression (mRNA) and increases bone density/volume and mineralization in vivo.

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

INF39 is a noncytotoxic and irreversible NLRP3 inhibitor.

GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells[1]. GSK717 blocks synergy between NOD2 and TLR2. GSK717 does not affect NOD1, TNFR1 and TLR2-mediated responses. GSK717 (5 μM) inhibits the release of IL-8, IL-6, TNFα and IL-1β in primary human monocytes stimulated with MDP[1]. [1]. Rickard DJ, et al. Identification of benzimidazole diamides as selective inhibitors of the nucleotide-binding oligomerization domain 2 (NOD2) signaling pathway. PLoS One. 2013;8(8):e69619. Published 2013 Aug 1.

CY-09 is an NLRP3 inhibitor.

NLRP3/AIM2-IN-3 is a unique molecule that inhibits NLRP3 and AIM2 inflammasome activation in a species-specific manner. It has an IC50 value for cell lysis of 0.077 ± 0.008 μ M. NLRP3/AIM2-IN-3 is a potent inhibitor of NLRP3 and AIM2 inflammasome-dependent cell lysis with an IC50 value for cell lysis of 0.077 ± 0.008 μ M. NLRP3/AIM2-IN-3 inhibits LPS/nigericin NLRP3/AIM2-IN-3 inhibits LPS/nigericin-stimulated cell lysis in THP-1 macrophages with an IC50 value of 0.077 ± 0.008 μM. NLRP3/AIM2-IN-3 interferes with the interaction of NLRP3 or AIM2 with the bridging protein ASC, inhibiting oligomerization of ASC.

Physalin B is one of the major active compounds from the Solanaceae family of plants and has a wide range of biological activities for the treatment of inflammatory eczema and herpes, among other diseases.Physalin B ameliorates lipopolysaccharide-induced inflammatory response due to acute lung injury by inhibiting NF-κB and NLRP3 through activation of the PI3K/Akt pathway.Physalin B inhibits PDGF-BB-induced VSMC proliferation and migration and phenotypic transformation through activation of the Nrf2 pathway. Physalin B inhibits PDGF-BB-induced VSMC proliferation, migration and phenotypic transformation through activation of the Nrf2 pathway.Physalin B exerts antitumor activity by inhibiting LAP2α-HDAC1-mediated deacetylation of glioma-associated oncogene 1 and hepatic stellate cell activation.

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

NLRP3-IN-9 (INF-4E) is an inhibitor of NLRP3 ATPase and caspase-1. NLRP3-IN-9 acts by irreversibly trapping thiol nucleophiles, which prevents both ATP- and nigericin-triggered pyroptosis of human THP-1 cells in a time- and concentration-dependent manner.

Asymmetric dimethylarginine is an endogenous inhibitor of nitric oxide synthase (NOS)

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

Procyanidin B2 (Proanthocyanidin B2) has vascular protective, anti-diabetic nephropathy, anti-cancer, anti-inflammatory, and antioxidant activities. Procyanidin B2 inhibited NLRP3 inflammasome activation via suppression of AP-1 pathway.