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。
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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 | ✔ | HDAC,Nrf2 | 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。 |
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 | |
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. |
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 |
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 |