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BAY 11-7085 {[allProObj[0].p_purity_real_show]}

货号:A252603 同义名: BAY 11-7083

BAY 11-7085 (BAY 11-7083) 是一种 NF-κB 活化和 IκBα 磷酸化抑制剂,稳定 IκBα 的 IC50 为 10 μM。

BAY 11-7085 化学结构 CAS号:196309-76-9
BAY 11-7085 化学结构
CAS号:196309-76-9
BAY 11-7085 3D分子结构
CAS号:196309-76-9
BAY 11-7085 化学结构 CAS号:196309-76-9
BAY 11-7085 3D分子结构 CAS号:196309-76-9
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BAY 11-7085 纯度/质量文件 产品仅供科研

货号:A252603 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 NF-κB 其他靶点 纯度
PDTC ammonium 98%
QNZ ++++

NF-κB, IC50: 11 nM

99%+
Sodium 4-Aminosalicylate Dihydrate 98%
Sodium Salicylate 95%
Parthenolide p53 97% HPLC
JSH-23 +

NF-κB, IC50: 7.1 μM

98%
Phenethyl caffeate 98%
Andrographolide 98+%
Curcumin Nrf2,HDAC 98%
SC75741 +++

NF-κB, EC50: 200 nM

99%+
CBL0137 HCl ++

NF-κB, EC50: 0.47 μM

p53 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

BAY 11-7085 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.

BAY 11-7085 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
human HT-29 cells Function assay 30 mins Reduction of cellular GSH level in human HT-29 cells incubated for 30 mins followed by co-culturing with human mesothelial cells measured after 5 hrs by firefly luciferase assay 25581261

BAY 11-7085 动物研究

Dose Mice: 3 mg/kg, 10 mg/kg[3] (i.p.), 20 mg/kg[4] (i.p.) Rat: 20 mg/kg[5] (i.p.)
Administration i.p.

BAY 11-7085 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.

BAY 11-7085 实验方案

计算器
存储液制备 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

BAY 11-7085 技术信息

CAS号196309-76-9
分子式C13H15NO2S
分子量 249.33
别名 BAY 11-7083
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

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
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