Home NF-κB IκB/IKK inhibitor Bay 11-7085

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Bay 11-7085 IκB/IKK inhibitor

Cat.No.S7352

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

Chemical Structure

Molecular Weight: 249.33

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Quality Control

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

Cell Culture, Treatment & Working Concentration

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
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
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
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
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
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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 50 mg/mL (200.53 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 249.33 Formula

C13H15NO2S

 Storage (From the date of receipt)
CAS No. 196309-76-9 -- Storage of Stock Solutions

Synonyms Bay 11-7083 Smiles CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)C=CC#N

Mechanism of Action

Features
Selective IκBα phosphorylation inhibitor.
Targets/IC50/Ki
IκBα phosphorylation
10 μM
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. BAY 11-7085 enhances the inhibition of NFkappaB activity and decreases the viability of cells. Besides, combination of Bay11-7085 and LY294002 leads to synergistic apoptotic effect in PEL cells.

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.
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. BAY 11-7085 increases the efficacy of induced inhibition of intraabdominal dissemination and production of ascites in athymic nude mice bearing Caov-3 cells.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/22768179/

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