BAY 11-7082 is a NF-κB inhibitor that selectively and irreversibly inhibits the TNF-α-inducible phosphorylation of IκBα (IC50=10 uM), also inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 uM and 0.96 uM, respectively.
BAY 11-7082 induces apoptosis of HTLV-I-infected T-cell lines but only negligible apoptosis of HTLV-I-negative T cells, rapidly and efficiently reduces the DNA binding of NF-κB in HTLV-I-infected T-cell lines and down-regulates the expression of the antiapoptotic gene, Bcl-xL, regulated by NF-κB.
BAY 11-7082 selectively inhibits Tax-induced NF-κB activity in a human T-cell line.
BAY 11-7082 exerts effects by inactivating the E2-conjugating enzymes Ubc (ubiquitin conjugating) 13 and UbcH7 and the E3 ligase LUBAC (linear ubiquitin assembly complex), thereby preventing the formation of Lys63-linked and linear polyubiquitin chains.
BAY 11-7082 prevents ubiquitin conjugation to Ubc13 and UbcH7 by forming a covalent adduct with their reactive cysteine residues.