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    Bay 11-7085
    Bay 11-7085

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0760
    CAS #: 196309-76-9Purity ≥98%

    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. It inhibits TNFα-induced IκBα phosphorylation with an IC50 of 10 μM. BAY117085 induces apoptosis of ovarian endometriotic cyst stromal cells/ECSCs by suppressing antiapoptotic proteins. Therefore, BAY 11-7085 has the potential to be used for the treatment of endometriosis.

    References: J Biol Chem. 1997 Aug 22;272(34):21096-103.

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    Molecular Weight (MW)249.33
    FormulaC13H15NO2S
    CAS No.196309-76-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 50 mg/mL (200.5 mM)
    Water: <1 mg/mL
    Ethanol: 50 mg/mL (200.5 mM)
    Other infoChemical Name: (2E)-3-[[4-(1,1-Dimethylethyl)phenyl]sulfonyl]-2-propenenitrile
    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+
    SMILES Code: N#C/C=C/S(=O)(C1=CC=C(C(C)(C)C)C=C1)=O
    SynonymsBay 11-7083; Bay 11-7085; Bay-11-7085; Bay11-7085; Bay 117085; Bay-117085; Bay117085; Bay-11-7083; Bay11-7083; 


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    In Vitro

    In vitro activity: 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 by paclitaxel and decreases the viability of cells treated with paclitaxel. Besides, combination of Bay11-7085 and LY294002 leads to synergistic apoptotic effect in PEL cells.


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

    In VivoBAY 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 paclitaxel-induced inhibition of intraabdominal dissemination and production of ascites in athymic nude mice bearing Caov-3 cells.
    Animal modelRat model of pneumococcal meningitis
    Formulation & DosageDissolved in PBS; 20 mg/kg; i.p. injection
    References

    J Infect Dis. 2000 Nov;182(5):1437-45; Clin Cancer Res. 2004 Nov 15;10(22):7645-54.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    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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