Information
BAY 11-7082 (BAY 11-7821) is aNF-κBinhibitor, inhibits TNFα-inducedIκBαphosphorylation withIC50of 10 μM in tumor cells. BAY 11-7082 inhibitsubiquitin-specific protease USP7andUSP21with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 inducesapoptosi
In vitro
BAY 11-7082 completely and specifically abrogates NF-κB DNA binding, downregulating the NF-κB-inducible cytokine IL-6 and inducing apoptosis. BAY 11-7082 (< 8 μM) is able to effectively inhibit both basal and TNFα stimulated NFκB luciferase activity in a dose dependent manner. BAY 11-7082 (8 μM) strongly inhibits the rate of proliferation in NCI-H1703 cells. Bay 11-7082 (5 μM) rapidly and efficiently reduces the DNA binding of NF-kappaB in HTLV-I-infected T-cell lines and down-regulates the expression of the antiapoptotic gene, Bcl-x(L), whereas it has little effect on the DNA binding of another transcription factor, AP-1. Bay 11-7082-induced apoptosis of primary ATL cells is more prominent than that of normal peripheral blood mononuclear cells, and apoptosis of these cells is also associated with down-regulation of NF-kappaB activity. Bay 11-7082 (5 μM) selectively induces apoptosis of HTLV-I–infected T-cell lines associated with down-regulation of the expression of cyclin D1, cyclin D2, and Bcl-xL. BAY 11-7082 (100 μM) prevents the nuclear translocation of p65 elicited by NMDA and the NMDA-induced increase of NF-κB binding in mouse hippocampal slices. BAY 11-7082 prevents NMDA toxicity occurring in CA1 region of hippocampal slices with 40% neuroprotection at 20 μM and 70% neuroprotection at 100 μM. BAY 11-7082 at all concentrations tested significantly inhibits NF-κB p65 DNA-binding activity in adipose tissue, whereas in skeletal muscle, BAY 11-7082 at 50 μM and 100 μM significantly inhibits NF-κB p65 DNA-binding activity. BAY 11-7082 (100 μM) reduces IKK-β protein in human adipose tissue and skeletal muscle. BAY 11-7082 (100 μM) significantly decreases the release of TNF-α from adipose tissue, whereas the release of IL-6 and IL-8 is significantly inhibited at all concentrations of BAY 11-7082 tested. BAY 11-7082 (50 μM) significantly decreases the release of TNF-α, IL-6, and IL-8 in skeletal muscle. BAY 11-7082 is also found to inactivate the E2-conjugating enzymes Ubc (ubiquitin conjugating) 13 and UbcH7 and the E3 ligase LUBAC (linear ubiquitin assembly complex), and thus induces B-cell lymphoma and leukaemic T-cell death. [6]
In vivo
Cell Data
cell lines：
Concentrations：~8 μM
Incubation Time：12 hours
Powder Purity:≥99%
L2214598