product name Bay 11-7085
Description: BAY 11-7085 is a soluble, irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM. BAY 11-7085 has been shown to inhibit cell proliferation and induce apoptosis of a variety of cells. BAY 11-7085 induces apoptosis of ECSCs by suppressing antiapoptotic proteins, and that caspase-3-, -8-, and -9-mediated cascades are involved in this mechanism. BAY 11-7085 could be used as a therapeutic agent for the treatment of endometriosis. BAY 11-7085 protects against gut ischemia-reperfusion injury.
References: J Biol Chem. 1997 Aug 22;272(34):21096-103.
249.33
Formula
C13H15NO2S
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)
Solubility (In vivo)
Synonyms
Bay 11-7083
other peoduct :
| 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 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 paclitaxel-induced inhibition of intraabdominal dissemination and production of ascites in athymic nude mice bearing Caov-3 cells. |
| Animal model | Rat model of pneumococcal meningitis |
| Formulation & Dosage | Dissolved 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. |
