Home NF-κB IκB/IKK inhibitor Bay 11-7085 For research use only.

Bay 11-7085

Synonyms: Bay 11-7083

BAY 11-7085 (Bay 11-7083) is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.

Bay 11-7085 Chemical Structure

Bay 11-7085 Chemical Structure

CAS No. 196309-76-9

Purity & Quality Control

Batch: S735201 DMSO]50 mg/mL]false]Ethanol]50 mg/mL]false]Water]Insoluble]false Purity: 99.87%
99.87

Bay 11-7085 Related Products

Signaling Pathway

IκB/IKK Signaling Pathways

IκB/IKK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa cells Function assay Inhibition of IL-1-alpha-induced NF-kappaB activation in HeLa cells assessed as blocking of p50/p65 nuclear translocation, IC50=0.1 μM 17845850
human A2780 cells Function assay Antitumor activity against human A2780 cells co-cultured with mesothelial cell monolayers by firefly luciferase reporter gene assay, IC50=2.6 μM 22326395
human BxPC3 cells Cytotoxicity assay 4 h Cytotoxicity against human BxPC3 cells co-cultured with human mesothelial cells after 4 hrs by firefly luciferase assay relative to control, EC50=3.5 μM 25581261
human SKOV3 cells Cytotoxicity assay 4 h Cytotoxicity against human SKOV3 cells co-cultured with human mesothelial cells after 4 hrs by firefly luciferase assay relative to control, EC50=5 μM 25581261
human SU86 cells Cytotoxicity assay 4 h Cytotoxicity against human SU86 cells co-cultured with human mesothelial cells after 4 hrs by firefly luciferase assay relative to control, EC50=5.9 μM 25581261
human HT-29 cells Function assay 30 mins Reduction of cellular GSH level in human HT-29 cells incubated for 30 mins followed by co-culturing with human mesothelial cells measured after 5 hrs by firefly luciferase assay 25581261
Click to View More Cell Line Experimental Data

Biological Activity

Description BAY 11-7085 (Bay 11-7083) is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.
Features Selective IκBα phosphorylation inhibitor.
Targets
IκBα phosphorylation [1]
10 μM
In vitro
In vitro

BAY 11-7085 inhibits TNFα-induced expression of adhesion molecules E-selectin, VCAM-1, and ICAM-1 by inhibition of NF-κB without detectable cytotoxicity at 10 μM in HUVEC cells. [1] BAY 11-7085 enhances the inhibition of NFkappaB activity and decreases the viability of cells. [3] Besides, combination of Bay11-7085 and LY294002 leads to synergistic apoptotic effect in PEL cells. [4]
Kinase Assay In Gel Kinase Assay
In gel kinase assay for the proteins that phosphorylate IκB-α is carried out as detailed below. Whole cell extracts are prepared from HUVEC treated with TNFα (100 units/ml) for 15 min in the presence or absence of inhibitor (20 μM, pretreatment for 1 h) as indicated. Proteins are separated on a 10% SDS gel containing 0.5 mg/ml HIS-IκB-α. Gels are washed two times in 20% propanol, 50 mM Hepes, pH 7.6, for 30 min and two times in buffer A (50 mM Hepes, pH 7.6, 5 mM 2-mercaptoethanol) for 30 min, followed by a 1-h incubation with buffer A, 0.05% Tween 20 and 1 h in buffer A with 0.05% Tween 20. The kinase assay is carried out for 1 h at 30 °C in the presence of 50 μM ATP, 5 μCi/ml [32P]ATP, 20 mM Hepes, pH 7.6, 20 mM MgCl2, 20 mM β-glycerophosphate, 20 mM p-nitrophenyl phosphate, 1 mM sodium vanadate, 2 mM dithiothreitol. The gel is washed with 5% trichloroacetic acid and 1% sodium pyrophosphate, dried, and exposed to film. A separate gel with no HIS-IκB-α is assayed as a control.
Cell Research Cell lines HUVEC cells
Concentrations ~20 μM
Incubation Time 16 hours
Method

Human umbilical vein endothelial cells (HUVEC) are isolated and maintained in culture. Cell toxicity is assessed by morphology and by MTT assay.
In Vivo
In vivo

BAY 11-7085 inhibits the meningitis-associated increase in NF-κB activity, and results in an improvement of the clinical status of infected rats and a marked attenuation of meningitis-associated CNS complications and meningeal inflammation. [2] BAY 11-7085 increases the efficacy of induced inhibition of intraabdominal dissemination and production of ascites in athymic nude mice bearing Caov-3 cells. [3]
Animal Research Animal Models Rat model of pneumococcal meningitis
Dosages PBS
Administration i.p.

Chemical Information & Solubility

Molecular Weight 249.33 Formula

C13H15NO2S
CAS No. 196309-76-9 SDF --
Smiles CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)C=CC#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 50 mg/mL ( (200.53 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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