NOD-like Receptor (NLR) Inhibitor

NP3-146 is a NLRP3 inflammasome inhibitor through locking the NACHT domain of NLRP3. NP3-146 shows potent inhibitory activity against IL-1β release with an IC₅₀ value of 0.171 μM in LPS (HY-D1056)/Nigericin (HY-127019)-stimulated BMDM cells. NP3-146 regulates the levels of cleaved Caspase-1 and cleaved IL-1β in cell supernatants. NP3-146 can be used for the research of inflammatory diseases.

NLRP3-IN-26 (compound 15Z) is a NLRP3 inhibitor with the IC₅₀ of 0.13 μM. NLRP3-IN-26 can be used for DSS-induced colitis model study.

Ciliatoside A is a naturally bioactive compound that exhibits significant anti-inflammatory, antiviral, and neuroprotective activities. Ciliatoside A serves as a mitophagy inducer and NLRP3 inflammasome inhibitor, activating AMPK, SIRT1, and the PINK1/Parkin axis, and inhibiting pyroptosis and apoptosis. Ciliatoside A promotes autophagic flux, autophagosome-lysosome fusion, mTOR inhibition, and p62-dependent HBc degradation; reduces Aβ aggregation, plaque deposition, microglial/astrocyte activation, and bacterial load; and maintains neuronal integrity, mitochondrial membrane potential, and ATP production. Ciliatoside A is used in research on Alzheimer's disease, Klebsiella pneumoniae-induced pneumonia, hepatitis B virus infection, and inflammation.

NLRP3-IN-71 (Compound 19) is a BBB-permeable, orally active and selective NLRP3 inhibitor that can inhibit IL-1β secretion. NLRP3-IN-71 can be used for the research of neurodegenerative diseases.

RIPK2-IN-7 (Compound 10w) is an orally active, selective RIPK2 inhibitor (IC₅₀: 0.6 nM). RIPK2-IN-7 inhibits RIPK2 kinase activity, blocks the nucleotide-binding oligomerization domain (NOD) signaling pathway, and reduces the production of inflammatory factors (such as TNFα). RIPK2-IN-7 can be used in the study of inflammatory bowel disease (IBD).

NLRP3-IN-49 (compound Z48) is a potent and specific NLRP3 inhibitor (IC₅₀=0.26 μM in THP-1 cells, IC₅₀=0.21 μM in mouse bone marrow macrophages). NLRP3-IN-49 can directly bind to NLRP3 protein (K_d=1.05 μM), effectively preventing the assembly and activation of NLRP3 inflammasome, thereby exhibiting anti-inflammatory properties. NLRP3-IN-49 can be used in the study of inflammatory bowel disease.

NLRP3-IN-89 is a NOD-like receptor protein 3 (NLRP3) inflammasome inhibitor. NLRP3-IN-89 inhibits the NLRP3 inflammasome pathway, reduces IL-1β secretion, and exhibits minimal interference with the NF-κB pathway. NLRP3-IN-89 can be used for the research of Parkinson's disease, frontotemporal dementia, multiple system atrophy, Alzheimer's disease, multiple sclerosis, amyotrophic lateral sclerosis, or brain injury.

NP-1815-PX is an orally active dual inhibitor of P2X4 and prostaglandin TP receptors, with an IC₅₀ of 0.26 μM against human P2X4 receptors. NP-1815-PX specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX not only produces anti-allodynic effects in vivo, but also significantly alleviates symptoms of DNBS (HY-W324435)-induced colitis (such as weight loss and tissue damage). NP-1815-PX exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX is used in studies related to asthma and inflammatory bowel disease (colitis).

JNJ-79883960 is a NLRP3 inhibitor. JNJ-79883960 can be used for the study of inflammation.

NLRP3-IN-12 is a specific NLRP3 inflammasome inhibitor. NLRP3-IN-12 reduces the release of IL-1β by targeting the NLRP3 protein, with an IC₅₀ of 0.45 μM. NLRP3-IN-12 can be used for the research of inflammatory bowel disease.

NLRP3-IN-65 (compound 41) is a potent NLRP3 inhibitor.

NLRP3-IN-73 (W16) is an orally active inhibitor of the assembly of NLRP3 inflammasome via targeting NLRP3, with an IC₅₀ value of 0.18 μM for the NLRP3/IL-1β pathway.

NLRP3-IN-4 is potent and orally active NLRP3 inflammasome inhibitor with inflammatory activity for colitis.

NOD1 Human Pre-designed siRNA Set A contains three designed siRNAs for NOD1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

MBL-1 is an orally active anti-inflammatory agent. MBL-1 can be isolated from the fermentation broth of Aspergillus sp. derived from gorgonians. MBL-1 inhibits the activity of the hCOX-2 protein with an IC₅₀ of 5.77 μM. MBL-1 reduces the production of key pro-inflammatory mediators such as NO, ROS, IL-1β and IL-18 by inhibiting the MAPK/NF-κB and NLRP3 signaling pathways. MBL-1 exerts a protective effect against DSS-induced colitis. MBL-1 can be used for the research of ulcerative colitis.

NLRP3-IN-60 (Compound 39) is the orally active inhibitor for NLRP3. NLRP3-IN-60 inhibits pyroptosis with an IC₅₀ of 13 nM in THP-1 cell. NLRP3-IN-60 inhibits IL-1β release with an IC₅₀ of 225 nM in human whole blood.

NLRP3-IN-76 is an orally active NLRP3 inhibitor. NLRP3-IN-76 inhibits the production of NO, and the mRNA levels of proinflammatory cytokines (iNOS, IL-6, IL-1β and TNFα). NLRP3-IN-76 shows anti-inflammatory effects by inhibiting the activation of the NLRP3 inflammasome and NF-κB signaling pathway. NLRP3-IN-76 ameliorates DSS (HY-116282C)-induced colitis and can be used for research of inflammatory bowel diseases (IBD).

NLRP3-IN-64 (Compound 2) is an inhibitor for NLRP3, that inhibits the NLRP3 activation with an EC₅₀ of 5 nM.

XB2M54 is a selective XIAP antagonist. XB2M54 inhibits NOD2-mediated inflammatory signaling. XB2M54 is an E3 ligase ligand. XB2M54 can be used for synthesis of PROTAC ERα Degrader-1 (HY-112098).

NQO2 activator-1 (Compound 1d) is a selective NQO2 activator with 20.89% increase of NQO2 activity at 10 μM. NQO2 activator-1 strongly inhibits NLRP3 inflammasome activation. NQO2 activator-1 can be used for the research of inflammation and immunology, such as rheumatoid arthritis.