|(E)-3-((4-(叔丁基)苯基)磺酰基)丙烯腈|CsnPharm

CAS No.: 196309-76-9

BAY 11-7085 Catalog No. CSN13625

Synonyms: BAY 11-7083;BAY 11-7085BAY 11-7085BAY 11-7085

BAY 11-7085 is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 IκBα phosphorylation

IC50:10μM
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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
动物研究
剂量
Mice: 3 mg/kg, 10 mg/kg^[3] (i.p.), 20 mg/kg^[4] (i.p.) Rat: 20 mg/kg^[5] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 3 mg/kg, 10 mg/kg^[3] (i.p.), 20 mg/kg^[4] (i.p.) Rat: 20 mg/kg^[5] (i.p.)
给药途径	i.p.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.0107 mL
- 20.0537 mL
- 40.1075 mL
- 5 mM
- 0.8021 mL
- 4.0107 mL
- 8.0215 mL
- 10 mM
- 0.4011 mL
- 2.0054 mL
- 4.0107 mL

技术信息

CAS号

196309-76-9

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H15NO2S

运输

蓝冰

分子量

249.33

别名

BAY 11-7083;BAY 11-7085BAY 11-7085BAY 11-7085

溶解度

DMSO	50.0 mg/mL (200.5 mM)
Water	Insoluble
Ethanol	50.0 mg/mL (200.5 mM)

动物实验配方

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