Bay 11-7085

Alias: Bay 11-7083; Bay 11-7085; Bay-11-7085; Bay11-7085; Bay 117085; Bay-117085; Bay117085; Bay-11-7083; Bay11-7083
Cat No.:V0760 Purity: ≥98%
BAY 11-7085 (BAY-11-7085; BAY 117085) is a novel, potent, soluble, irreversible inhibitor of TNFα-induced IκBα phosphorylation with potential anticancer activity.
Bay 11-7085 Chemical Structure CAS No.: 196309-76-9
Product category: IκB IKK
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

BAY 11-7085 (BAY-11-7085; BAY 117085) is a novel, potent, soluble, irreversible inhibitor of TNFα-induced IκBα phosphorylation with potential anticancer activity. With an IC50 of 10 μM, it prevents TNFα-induced IκBα phosphorylation. By inhibiting antiapoptotic proteins, BAY117085 causes ovarian endometriotic cyst stromal cells/ECSCs to undergo apoptosis. Consequently, BAY 11-7085 may be employed in the management of endometriosis.

Biological Activity I Assay Protocols (From Reference)
Targets
NF-κB; IκB-α (IC50 = 10 μM)
ln Vitro
BAY 11-7085 inhibits TNFa-induced surface expression of E-selectin, VCAM-1, and ICAM-1with IC50 values in the range of 5-10 μM. With an IC50 value of roughly 10 μM, BAY 11-7085 dose-dependently stabilizes IκBα . There is a direct correlation between the drug concentration that stabilized IκBα, the concentration that inhibits nuclear NF-kB levels, and the concentration that inhibits adhesion molecule expression[1].
It has been demonstrated that BAY 11-7085 causes a variety of cells to undergo apoptosis and inhibits cell proliferation. Cell proliferation and DNA synthesis in ovarian endometriotic cyst stromal cells are significantly reduced by BAY 11-7085 (ECSCs), which also causes apoptosis and the arrest of these cells' cell cycle in the G0/G1 phase. By suppressing antiapoptotic proteins, BAY 11-7085 causes ECSCs to undergo apoptosis, and caspase-3, -8, and -9-mediated cascades are involved in this mechanism[2].
ln Vivo
In the rat carrageenan paw model and the rat adjuvant arthritis model, BAY 11-7085 acts as an anti-inflammatory drug. The rat carrageenan paw model exhibits a dose-dependent decrease in swelling[1].
Enzyme Assay
The procedures for the gel kinase assay are described below for determining which proteins phosphorylate IκB-α . From HUVEC that have been exposed to TNFα (100 units/ml) for 15 minutes in the presence or absence of the inhibitor (20 μM, pretreatment for 1 hour), as indicated, whole cell extracts are made. A 10% SDS gel with 0.5 mg/ml HIS-IκB-α is used to separate proteins. 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 containing 6 M urea, 1 h each in 3, 1.5, and 0.75 M urea in buffer A and 0.05% Tween 20 and 1 h in buffer A with 0.05% Tween 20. The kinase assay is conducted for 1 hour at 30 °C with 50 μM ATP, 5 Ci/ml [32P]ATP, 20 mM Hepes, pH 7.6, 20 mM MgCl2, 20 mM -glycerophosphate, 20 mM p-nitrophenyl phosphate, 1 mM sodium vanadate, and 2 mM dithiothreitol present. The gel is dried, exposed to film, and then washed with 5% trichloroacetic acid and 1% sodium pyrophosphate. A different gel devoid of HIS-IκB-α is tested as a control.
Cell Assay
ECSCs cells are incubated with BAY 11-7085 (0.01 to 10 μM) for 48 hours. Then, each well receives 20 μL of WST-1 dye, and the cells are incubated for an additional 4 hours. Every experiment is carried out with 10% FBS present. Absorbance at 540 nm is used to assess cell proliferation[2].
Animal Protocol
Rats: Rats receive 0.1 mL of 1% suspension of carrageenan in distilled water as a subplantar injection into the footpad of the right hind paw. Rats receive either a fine suspension of compound 2 (1, 5 or 50 mg/kg) in vehicle or vehicle (polyethylglycol 400 diluted 1:5 in 5% bovine serum albumin/water) intraperitoneally for one hour prior to injection. Rats pretreated with 20 mg/kg of ibuprofen are part of a positive control group that is also present. The injection volume of the paw is measured four hours after carrageenan administration. Edema volume is calculated[1].
References

[1]. Novel inhibitors of cytokine-induced IkappaBalpha phosphorylation and endothelial cell adhesionmolecule expression show anti-inflammatory effects in vivo. J Biol Chem. 1997 Aug 22;272(34):21096-103.

[2]. Application of the nuclear factor-kappaB inhibitor BAY 11-7085 for the treatment of endometriosis: an in vitro study. Am J Physiol Endocrinol Metab. 2007 Jul;293(1):E16-23.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C13H15NO2S
Molecular Weight
249.33
Exact Mass
249.08
Elemental Analysis
C, 62.63; H, 6.06; N, 5.62; O, 12.83; S, 12.86
CAS #
196309-76-9
Appearance
White to off white solid powder
SMILES
CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)/C=C/C#N
InChi Key
VHKZGNPOHPFPER-ONNFQVAWSA-N
InChi Code
InChI=1S/C13H15NO2S/c1-13(2,3)11-5-7-12(8-6-11)17(15,16)10-4-9-14/h4-8,10H,1-3H3/b10-4+
Chemical Name
(E)-3-(4-tert-butylphenyl)sulfonylprop-2-enenitrile
Synonyms
Bay 11-7083; Bay 11-7085; Bay-11-7085; Bay11-7085; Bay 117085; Bay-117085; Bay117085; Bay-11-7083; Bay11-7083
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~50 mg/mL (~200.5 mM)
Water: <1 mg/mL
Ethanol: ~50 mg/mL (~200.5 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.0107 mL 20.0537 mL 40.1075 mL
5 mM 0.8021 mL 4.0107 mL 8.0215 mL
10 mM 0.4011 mL 2.0054 mL 4.0107 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Biological Data
  • Bay 11-7085

    Effect of BAY 11-7085 on paclitaxel-induced phosphorylation and degradation of IκBα, and on NFκB activity.Clin Cancer Res.2004 Nov 15;10(22):7645-54.
  • Bay 11-7085

    Effect of BAY 11-7085 on the expression of survival genes.Clin Cancer Res.2004 Nov 15;10(22):7645-54.
  • Bay 11-7085

    BAY 11-7085 enhances paclitaxel-induced attenuation of invasion.Clin Cancer Res.2004 Nov 15;10(22):7645-54.
  • Bay 11-7085

    Appearance and ascites formation of mice after treatment with paclitaxel, BAY 11-7085 alone, or the combination thereof.Clin Cancer Res.2004 Nov 15;10(22):7645-54.
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