BAY 11-7082

The transcription factor NF-?B plays a key role in regulating over 150 target genes including the expression of inflammatory cytokines, chemokines, immunoreceptors, and cell adhesion molecules.{13643} In the cytoplasm, inactive NF-?B complexes are bound to an inhibitor I?B.{12959} However in response to certain stimuli, I?B is phosphorylated, ubiquitinated, and degraded, enabling the translocation of NF-?B to the nucleus.{13642} BAY 11-7082 selectively and irreversibly inhibits NF-?B activation by blocking TNF-?-induced phosphorylation of I?B-? without affecting constitutive I?B-? phosphorylation.{16037} This compound inhibits the TNF-?-induced surface expression of adhesion molecules ICAM-1, VCAM-1, and E-selectin in human endothelial cells with IC50 values of 5-10 µM.{16037}