计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
金雀异黄酮, CFTR 激活剂;雌激素受体-β 激动剂;雌激素相关受体-α 激动剂;雌激素相关受体-β 激动剂;雌激素相关受体-γ 激动剂;TAS2R14 激动剂;TAS2R39 激动剂;TRPC5 激活剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 143 篇同行评审文献引用。
概述
溶于乙醇和DMSO， 干冷处保存。
Information
Genistein (NPI 031L), a phytoestrogen found in soy products, is a highly specific inhibitor ofprotein tyrosine kinase (PTK)which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells withIC50of 12μM or by insulin withIC50of 19 μM.
In vitro
Genistein is an ATP competitive inhibitor. Genistein inhibits tyrosine phosphorylation in isolated enzyme and receptor preparations and in whole cells including platelets, lymphocytes and a variety of cultured cells. It also inhibits EGF-stimulated phosphorylation in cultured cells as well as inhibition of Topo II (topoisomerase II). Genistein inhibits EGF-stimulated tyrosine phosphorylation in cultured A431 epidermoid carcinoma cells. Inhibition is competitive with ATP and noncompetitive with substrate. Genistein blocks the mitogenic effect mediated by EGF, insulin and thrombin on NIH-3T3 cells. Genistein also acts as an agonist at the GPR30 receptor and binds to PPARγ and estrogen receptors. Genistein also binds to PPARγ, acting as an agonist at this receptor with Ki of 5.7 μM.
In vivo
Genistein has chemopreventive effects on breast, prostate, and other endocrine-dependent tumors in adult animals. Genistein in the diet reduced the incidence of poorly differentiated prostatic adenocarcinomas in a dose-dependent manner and down-regulated androgen receptor, estrogen receptor-alpha, progesterone receptor, epidermal growth factor receptor, insulin-like growth factor-I, and extracellular signal-regulated kinase-1 but not estrogen receptor-beta and transforming growth factor-alpha mRNA expressions. Dietary genistein protects against mammary and prostate cancers by regulating specific sex steroid receptors and growth factor signaling pathways. Genistein combined with prostate tumor irradiation causes greater inhibition of primary tumor growth and increases control of spontaneous metastasis to para-aortic lymph nodes, increasing mouse survival. Paradoxically, treatment with genistein alone increases metastasis to lymph nodes.
Cell Data
cell lines：RL, H9, SKI, HBL-2, Granta and JJN-3 cell lines
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
英文别名
5,7-dihydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Genistein (NPI 031L)
生化机理
染料木素（NPI 031L）是豆制品中的一种植物雌激素，是一种高度特异性的蛋白酪氨酸激酶（PTK）抑制剂，它能阻断 EGF 对 NIH-3T3 细胞介导的有丝分裂效应，IC50 为 12 μM 或胰岛素介导的有丝分裂效应，IC50 为 19 μM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
激动剂
作用机制
CFTR 激活剂;雌激素受体-β 激动剂;雌激素相关受体-α 激动剂;雌激素相关受体-β 激动剂;雌激素相关受体-γ 激动剂;TAS2R14 激动剂;TAS2R39 激动剂;TRPC5 激活剂
名称和识别符
EC号
207-174-9
分子类型
小分子
Isomeric SMILES
C1=CC(=CC=C1C2=COC3=CC(=CC(=C3C2=O)O)O)O
分子量
270.24
Beilstein号
263823
Reaxy-Rn
263823
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=263823&ln=
技术文档
高级数据
关联靶点（人）
DPP4
Tclin
二肽基肽酶4(Dipeptidyl peptidase 4)
(1 活性数据)
ESRRA
Tchem
类固醇激素受体 ERR1(Steroid hormone receptor ERR1)
(1 活性数据)
ESR1
Tclin
雌激素受体(Estrogen receptor)
(6 活性数据)
ESR2
Tclin
雌激素受体β(Estrogen receptor beta)
(27 活性数据)
AOX1
Tchem
醛氧化酶(Aldehyde oxidase)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 46 mg/mL (198.03 mM);
熔点
297-298°C
安全和危险性（GHS）
WGK Germany
3
RTECS
NR2392000
Merck Index
4391
个人防护装备
Eyeshields,Faceshields,Gloves,type N95 (US),type P1 (EN143) respirator filter
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
Hedgehog信号通路
目录： 技术文章
Isoflavones
目录： 技术文章
Benzopyran Family at a Glance: From the Core Scaffold to Three High-Frequency Applications (Photochromism / Drug Scaffolds / Fluorescence) — with Product Selection Logic and Product Tables (Tables 1–3)
目录： 技术文章
Flavones: Structural Features, Physicochemical Properties, and Key Points for Research and Applications
目录： 技术文章
Mechanisms of Gut Microbial Enzyme-Mediated Metabolism of Glucuronide Conjugates and Drug Biotransformation
目录： 技术文章
黄酮类化合物提取方法及工艺选择
目录： 技术文章
Mechanisms by Which Flavonoid Natural Products Regulate the Oxidative Stress-Inflammation Axis
目录： 技术文章
天然产物调控脂肪褐变的分子机制
目录： 技术文章
此产品的引用文献
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
Copyright © 2023至今 上海阿拉丁生化科技股份有限公司 保留所有权利。
危险品化学品经营许可证（带存储）