BAY 11-7082 是一种 NF-Κb 抑制剂，可抑制 TNFα 诱导的 IκBα 磷酸化。 它抑制泛素特异性蛋白酶 USP7 和 USP21。

BAY 11-7082, a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21.

在NCI-H1703细胞中, BAY 11-7082（8 μM）能够抑制细胞增殖。在HTLV-I感染的T细胞系中,Bay 11-7082（5 μM）能够抑制NF-κB的DNA结合,并下调抗凋亡基因Bcl-x（L）的表达。在选择性诱导HTLV-1感染的T细胞系中, Bay11-7082（5 μM）能够引起细胞凋亡。在小鼠海马切片中,BAY 11-7082（100 μM）抑制NMDA诱导的NF-κB结合的增加,同时阻止NMDA引起的p65核转位。在骨骼肌中,BAY 11-7082（50-100 μM）显着抑制NF-κBp65 DNA结合活性。

UBE1 (0.17 μM) in 22.5 μL of 20 mM Hepes, pH 7.5, containing 10 μM ubiquitin is incubated for 45 min at 21°C with 1 μL of DMSO or 1 μL of BAY 11-7082 in DMSO. A 2.5 μL solution of 10 mM magnesium acetate and 0.2 mM ATP is added, incubated for 10 min at 30°C, and the reactions are terminated by the addition of 2.5 μL of 10% (w/v) SDS and heating for 6 min at 75°C. The samples are subjected to SDS/PAGE in the absence of any thiol. The gels are stained for 1 h with Coomassie Instant Blue and destained by washing with water. The loading of ubiquitin to E2 conjugating enzymes is carried out in an identical manner, except that UBE1 (0.17 μM) is mixed with Ubc13 (2.4 μM) or UbcH7 (2.9 μM) prior to incubation with BAY 11-7082[3].

Cells are transfected with siRNA in 96-well microtiter plates and then cultured for 72 hours in complete NSCLC medium, treated with BAY 11-7082 for 12 hours. Cells are incubated with [3H]thymidine for 3 hours. The cells are collected on filters using an automatic cell harvester and radioactivity on the filters is measured by β-scintillation counting.(Only for Reference)

19542-67-7

C10H9NO2S

207.25

BAY 11-7821

Ethanol:5.2 mg/mL (25 mM)
DMSO:20.7 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years