NF-κB (nuclear factor kappa B) is an intracellular protein complex that controls gene transcription, which was identified by D. Baltimore et al. in 1986.1) NF-κB is usually sequestered in the cytoplasm by forming an inactivated complex with IκB (Inhibitor κB). IKK (IκB kinase) activated by extracellular signals phosphorylates IκBα, and then the proteasome degrades phosphorylated IκBα. Then NF-κB can translocate into the nucleus and induce the expression of genes encoding molecules related to inflammatory immune response, apoptosis-suppressing molecules, cytostatic molecules, etc.2)
BAY 11-7082 is a small molecule inhibiting the phosphorylation of IκBα by IKK.3) It has been reported to use BAY 11-7082 as a NF-κB inhibitor in research of cancer, inflammation, viral infection and so on.4-7)
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An Inhibitor against NF-κB, a Significant Transcription Factor in the Immune System
References
- 1)Inducibility of κ immunoglobulin enhancer-binding protein NF-κB by a posttranslational mechanism
- 2)The complexity of NF-κB signaling in inflammation and cancer
- 3)Novel inhibitors of cytokine-induced IκBα phosphorylation and endothelial cell adhesion molecule expression show anti-inflammatory effects in vivo
- 4)Bay 11-7082 inhibits transcription factor NF-κB and induces apoptosis of HTLV-I–infected T-cell lines and primary adult T-cell leukemia cells
- 5)Nuclear factor-κB inhibitors as sensitizers to anticancer drugs
- 6)Anti-inflammatory compounds parthenolide and Bay 11-7082 are direct inhibitors of the inflammasome
- 7)The effects of heat shock protein 90 inhibitors on apoptosis and viral replication in primary effusion lymphoma cells
