EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #73462_C
NF-κB通路抑制剂；稳定IκB
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总览
Butein（紫铆因）是一种植物多酚，四羟基查耳酮，可抑制核因子NF-κB（Yang et al; Pandey et al. 2007）。紫铆因已被证明能抑制TNF依赖性IκBα（NF-κB的抑制亚基）的磷酸化和降解（IC₅₀=38 μM；Orlikova et al.）。紫铆因还能抑制5-脂氧合酶（IC₅₀=0.01 μM；Sogawa et al.），恶性疟原虫的烯酰酰基载体蛋白还原酶（Ki=2.97 μM；Sharma et al.），血管紧张素转换酶（IC₅₀=0.73 mM；Bonesi et al.）和SRC激酶（Pandey et al. 2009）。
代谢
·以浓度依赖性方式抑制大鼠脑匀浆中铁诱导的脂质过氧化（Cheng et al.）。
癌症研究
·抑制TNF-α诱导的人肺腺癌H1299细胞侵袭（Pandey et al. 2007; Gupta et al.）。
·通过诱导G2/M期停滞，抑制人肝癌细胞系HepG2和Hep3B的生长（Moon et al.; Gupta et al.）。
·抑制睾酮诱导的乳腺癌细胞增殖（Wang et al.）。
免疫学
·通过抑制LPS诱导的iNOS表达，在小鼠巨噬细胞系中表现出抗炎特性（Lee et al.）。
别名
2'，3，4，4'-四羟基查耳酮
细胞类型
癌细胞及细胞系，巨噬细胞
种属
人，小鼠，非人灵长类，其它细胞系，大鼠
研究领域
癌症，免疫，代谢
CAS 编号
487-52-5
化学式
C₁₅H₁₂O₅
分子量
272.3 克/摩尔
纯度
≥ 95 %
通路
NF-κB
靶点
IκB
产品说明书及文档
请在《产品说明书》中查找相关支持信息和使用说明，或浏览下方更多实验方案。
相关材料与文献
文献 (12)
Natural chalcones as dual inhibitors of HDACs and NF-κB. Oncology reports 2012 SEP
Abstract
Histone deacetylase enzymes (HDACs) are emerging as a promising biological target for cancer and inflammation. Using a fluorescence assay, we tested the in vitro HDAC inhibitory activity of twenty-one natural chalcones, a widespread group of natural products with well-known anti-inflammatory and antitumor effects. Since HDACs regulate the expression of the transcription factor NF-κB, we also evaluated the inhibitory potential of the compounds on NF-κB activation. Only four chalcones, isoliquiritigenin (no. 10), butein (no. 12), homobutein (no. 15) and the glycoside marein (no. 21) showed HDAC inhibitory activity with IC50 values of 60-190 µM, whereas a number of compounds inhibited TNFα-induced NF-κB activation with IC50 values in the range of 8-41 µM. Interestingly, three chalcones (nos. 10, 12 and 15) inhibited both TNFα-induced NF-κB activity and total HDAC activity of classes I, II and IV. Molecular modeling and docking studies were performed to shed light into dual activity and to draw structure-activity relationships among chalcones (nos. 1-21). To the best of our knowledge this is the first study that provides evidence for HDACs as potential drug targets for natural chalcones. The dual inhibitory potential of the selected chalcones on NF-κB and HDACs was investigated for the first time. This study demonstrates that chalcones can serve as lead compounds in the development of dual inhibitors against both targets in the treatment of inflammation and cancer.
Regulation of survival, proliferation, invasion, angiogenesis, and metastasis of tumor cells through modulation of inflammatory pathways by nutraceuticals. Cancer metastasis reviews 2010 SEP
Abstract
Almost 25 centuries ago, Hippocrates, the father of medicine, proclaimed Let food be thy medicine and medicine be thy food." Exploring the association between diet and health continues today. For example�
The synthesis and angiotensin converting enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives. Bioorganic & medicinal chemistry letters 2010 MAR
Abstract
A series of chalcones (1-9) and pyrazoles (10-18) was prepared to investigate their potential activity as Angiotensin I-Converting Enzyme (ACE) inhibitors. Their structures were verified by elemental analysis, UV, IR, MS, (1)H NMR, (13)C NMR, and 2D NMR experiments. Among tested compounds, chalcone 7 exerted the highest activity with an IC(50) value of 0.219 mM, while the most potent pyrazole was 15 (IC(50) value of 0.213 mM).
更多信息
| Molecular Weight | 272.3 g/mol |
|---|---|
| 种属 | Human, Mouse, Non-Human Primate, Other, Rat |
| Alternative Names | 2', 3, 4, 4'-Tetrahydroxychalcone |
| Cas Number | 487-52-5 |
| Chemical Formula | C₁₅H₁₂O₅ |
| 纯度 | ≥ 95% |
| Target | IκB |
| Pathway | NF-κB |
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