NOD

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

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.

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. It indirectly decreases osteoclast differentiation by reducing the RANKL OPG ratio and directly increases osteoblast differentiation by up-regulating Runx2 gene expression through MAPK pathways, thereby inducing bone formation via Runx2.

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.

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

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

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.

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

NT-0796 is a brain-permeable, potent, and selective inhibitor of the inflammasome NLRP3, inhibiting NLRP3 activation.NT-0796 is a potential NDT-19795 delivery vector.

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.

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

CY-09 is an NLRP3 inhibitor.

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

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.

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.

Asymmetric dimethylarginine [an endogenous inhibitor of nitric oxide synthase (NOS)], is a compound that inhibits the enzyme responsible for producing nitric oxide.

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.

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.

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.

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

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.

GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor that 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]. It blocks the synergy between NOD2 and TLR2 without affecting NOD1, TNFR1, and TLR2-mediated responses. At 5 μM, GSK717 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.

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

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

INF39 is a noncytotoxic and irreversible NLRP3 inhibitor.

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.

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.

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.

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.

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

NLRP3-IN-13 is a selective NLRP3 inhibitor that inhibits NLRP3-associated inflammation.NLRP3-IN-13 can be used in the study of neurological disorders and inflammation.

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).

NP3-146 (NLRP3-IN-5) is an inflammasome NLRP3 inhibitor with potential anti-inflammatory activity for the study of autoimmune diseases.

BAL-0028 is a potent inhibitor of NLRP3 activation (IC50: 25 nM) with anti-inflammatory activity for cancer research.

NLRP3 agonist 1 is an orally active and highly potent NLRP3 agonist that activates the enzyme Caspase-1, which may promote the maturation of pro-inflammatory cytokines.

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.

NT-0249 is an orally active inhibitor of the inflammatory vesicle NLRP3 with anti-inflammatory activity that reverses high-fat diet-induced obesity, systemic inflammation, and astrocyte hyperplasia.

INF 195 is an inflammasome NLRP3 inhibitor that inhibits NLRP3-driven macrophage pyroptosis and IL-1β release. INF 195 reduces isoproterenol-induced hypertrophy in H9c2 rat myoblasts and can be used to study myocardial ischemia and myocardial infarction.