BAY 11-7085

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Chemical Structure| 196309-76-9 同义名 : BAY 11-7083
CAS号 : 196309-76-9
货号 : A252603
分子式 : C13H15NO2S
纯度 : 99%+
分子量 : 249.33
MDL号 : MFCD01862602
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(100.27 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The NF-kB pathway plays a key role in multiple cellular processes, including immune signaling, inflammation, development, proliferation and survival. NF-κB suppression occurred through inhibition, activation, phosphorylation and degradation of IκB-α, p65 phosphorylation, p65 nuclear translocation, and NF-κB-mediated reporter gene transcription. BAY 11-7085 is an IκB-α inhibitor with IC50 value of <10μM for inhibiting the TNF-α-induced loss of IκB-α in HUVEC cells. Pre-treatment with BAY 11-7085 at concentration ranging in 1-20μM for 1h dose-dependently stabilized p-IκB-α and suppressed activation of NF-κB induced by TNF-α in HUVEC cells. Pre-treatment with 2.5-20μM BAY 11-7085 for 1h before 6-hour treatment with C pneumoniae could lead a concentration-dependent inhibition of C pneumoniae–induced ICAM-1 upregulation in human aortic endothelial cells. Combination of 5μM BAY 11-7085 with 200nM paclitaxel could attenuate the both basal and transient induction of IκBα phosphorylation by paclitaxel in Caov-3 cells, as well as decreased the viability of cells treated with paclitaxel. Administration of 5mg/kg BAY 11-7085 3 times weekly for 4 weeks could enhance paclitaxel (20 mg/kg, 3 times weekly)-induced inhibition of intraabdominal dissemination and production of ascites in athymic nude mice inoculated intraperitoneally with Caov-3 cells.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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 17845850
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 22326395
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 25581261
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.01mL

0.80mL

0.40mL

20.05mL

4.01mL

2.01mL

40.11mL

8.02mL

4.01mL
参考文献

[1]Mabuchi S, Ohmichi M, et al. Inhibition of inhibitor of nuclear factor-kappaB phosphorylation increases the efficacy of paclitaxel in in vitro and in vivo ovarian cancer models. Clin Cancer Res. 2004 Nov 15;10(22):7645-54.

[2]Pierce JW, Schoenleber R, et al. Novel inhibitors of cytokine-induced IkappaBalpha phosphorylation and endothelial cell adhesion molecule expression show anti-inflammatory effects in vivo. J Biol Chem. 1997 Aug 22;272(34):21096-103.