Antibodies
BAY 11-7085 is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.
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| Description | BAY 11-7085 is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM. | |||||
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| Targets | IκBα | |||||
| IC50 | 10 μM [1] | |||||
| 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 by paclitaxel and decreases the viability of cells treated with paclitaxel. [3]Besides, combination of Bay11-7085 and LY294002 leads to synergistic apoptotic effect in PEL cells. [4] | |||||
| 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 paclitaxel-induced inhibition of intraabdominal dissemination and production of ascites in athymic nude mice bearing Caov-3 cells. [3] | |||||
| Features | ||||||
| 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 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. |
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| Cell lines | HUVEC cells |
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| 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. |
| Animal Models | Rat model of pneumococcal meningitis |
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| Dosages | PBS |
| Administration | i.p. |
| Molecular Weight (MW) | 249.33 |
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| Formula | C13H15NO2S |
| CAS No. | 196309-76-9 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | Bay 11-7083 |
| Solubility (25°C) * | In vitro | DMSO | 50 mg/mL (200 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 50 mg/mL (200 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | (2E)-3-[[4-(1,1-Dimethylethyl)phenyl]sulfonyl]-2-propenenitrile |
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