Nuclear factor-κB (NF-κB) is an ubiquitous transcription factor that functions to enhance the transcription of pro-inflammatory cytokines like TNF-α, IL-1β, IL-6, and IL-8.1 QNZ is an inhibitor of NF-κB activation with an IC50 of 11 nM in human Jurkat cells. It also inhibits TNFα production from lipopolysaccharide-stimulated mouse splenocytes with an IC50 of 7 nM. QNZ showed efficacy in vivo by reducing edema formation in carrageenin-induced inflammation of rat hind paw.2
1
Karin, M., Yamamtoto, Y., and Wang, Q.M. The IKK NF-κB system: A treasure trove for drug development. Nat Rev Drug Discov317-26(2004).
2
Tobe, M., Isobe, Y., Tomizawa, H., et al. Discovery of quinazolines as a novel structural class of potent inhibitors of NF-κB activation. Bioorg Med Chem11383-391(2003).
Karin, M., Yamamtoto, Y., and Wang, Q.M. The IKK NF-κB system: A treasure trove for drug development. Nat Rev Drug Discov317-26(2004).
Tobe, M., Isobe, Y., Tomizawa, H., et al. Discovery of quinazolines as a novel structural class of potent inhibitors of NF-κB activation. Bioorg Med Chem11383-391(2003).
QNZ is available in the following screening
library: