NOD-like Receptor (NLR) Antagonist

NVP-DFV890 is an orally administered, selective NLRP3 inhibitor. NVP-DFV890 directly binds to NLRP3, blocks maturation of pro-inflammatory cytokines IL-1β and IL-18, and inhibits pyroptotic cell death. NVP-DFV890 acts as an inducer of viral clearance, promoting earlier clearance of SARS-CoV-2. NVP-DFV890 can be used for the research of COVID-19 pneumonia and coronavirus-associated acute respiratory distress syndrome (CARDS).

NLRP3 antagonist 1 is a potent antagonist of NLRP3. NLRP3 is mainly expressed in macrophages and neutrophils and is involved in the body's intrinsic immunity against pathogenic infections and stress injury. NLRP3 antagonist 1 has the potential for the research of cancer disease (extracted from patent WO2021114691A1, compound 3).

HDAC6-IN-54 (Compound 9m) is a highly selective HDAC6 (histone deacetylase 6) inhibitor with an IC₅₀ value of 0.021 μM. HDAC6-IN-54 blocks the activation of the NLRP3 inflammasome, which alleviates symptoms of NLRP3 inflammasome-related diseases such as acute peritonitis, inflammatory bowel disease, and psoriasis.

NOD1 antagonist-1 (compound 37) exhibits an antagonistic activity towards NOD1 and a weak NOD1/NOD2 selectivity, with IC₅₀s of 9.18 μM and 20.8 μM, respectively.

NOD1 antagonist-2 (compound 66) is an orally active selective antagonist of both human and mouse NOD1. NOD1 antagonist-2 (compound 66) antagonizes NOD1-induced NF-κB and MAPK pathways.

NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-binding oligomerization domain-like receptor 1/2) dual antagonist, with IC₅₀ values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T_1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX).

NOD1/2 antagonist-2 (Compound 26BH) is a dual NOD1/NOD2 antagonist (IC₅₀s: 2.36 μM and 4.16 μM for NOD1 and NOD2, respectively). NOD1/2 antagonist-2 inhibits both NF-κB and MAPK inflammatory signaling, thereby sensitizing Paclitaxel (HY-B0015) to suppress Lewis lung carcinoma growth.