nod-like receptor (nlr)

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 (CP-456773) is a NLRP3 inflammasome inhibitor (IC50=7.5-8.1 nM). MCC950 can be used to treat inflammatory diseases, inflammation-related tumors and neurodegenerative diseases.

Trimethylamine N-oxide (TMAO) is a gut microbiota-dependent metabolite derived from dietary choline, betaine, and carnitine. It induces inflammation by activating the ROS/NLRP3 inflammasome and promotes fibroblast differentiation through the activation of the TGF-β/Smad2 signaling pathway. TMAO is commonly used to induce cardiac fibrosis models.

CY-09 is an NLRP3 inhibitor.

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

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

Articaine hydrochloride (Hoe-045), a thiophene-containing local anesthetic, is pharmacologically similar to mepivacaine.

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

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.

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.

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.

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

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.

INF39 is a noncytotoxic and irreversible NLRP3 inhibitor.

1. Licochalcone B (LCB) inhibits the proliferation of human malignant bladder cancer cell lines (T24 and EJ) in vitro and antitumor activity in vivo in MB49 (murine bladder cancer cell line) tumor model. 2. LCB and Licochalcone D(LCD) significantly reduce

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

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

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.

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.

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.

CP 424174 is an inhibitor of IL-1β post-translational processing with IC50 of 210 nM. Inhibits the formation of mature IL-1β. Indirectly inhibits NLRP3. Active in vivo and orally bioavailable.

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

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