Stemcell, 73352, QNZ

QNZ is a quinazoline derivative that inhibits nuclear factor (NF)-κB activation (IC₅₀ = 11 nM in human Jurkat T lymphocyte cells). NF-κB enhances the transcription of pro-inflammatory cytokines, and QNZ inhibits lipopolysaccharide (LPS)-stimulated tumor necrosis factor (TNF)-α production in mouse splenocytes (IC₅₀ = 7 nM;Tobe et al.), as well as CXCL1-mediated pro-inflammatory increase in potassium currents in adult rat neurons (Yang et al). It does not inhibit kinases in a standard screen (Wu et al.).

MAINTENANCE

· Neuroprotective in a glutamate toxicity assay using YAC128 medium spiny neuron cultures (Wu et al.).

DISEASE MODELING

· Blocks amyloid precursor protein release in human SH-SY5Y neuroblastoma cells caused by muscarinic receptor activation (Choi et al.).