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金雀异黄酮

蛋白酪氨酸激酶抑制剂。抗癌剂。
规格或纯度: 97%
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货号 (SKU) 包装规格 是否现货 价格 数量
G106673-100mg
100mg 现货 Stock Image
G106673-500mg
500mg 现货 Stock Image
G106673-1g
1g 现货 Stock Image
G106673-5g
5g 现货 Stock Image
G106673-25g
25g 现货 Stock Image
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六元杂环化合物 苯丙素类

基本描述

别名 染料木素
英文别名 cid_5280961|GTPL2826|BRN 0263823|DH2M523P0H|MolMap_000022|GENISTEIN (USP-RS)|Differenol A|GENISTEIN [MI]|Genistein, analytical standard|Lopac0_000520|Oprea1_437815|5-18-04-00594 (Beilstein Handbook Reference)|Genistein (Standard)|Genisterin|KBio2_000800|K
规格或纯度 97%
英文名称 Genistein
生化机理 Description:
IC50 Value: 37.5 uM( Topo II) [3]
Genistein, a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM. It has been shown that genistein inhibits many type of cancers including prostate cancer (PCa) by regulating several cell signaling pathways and microRNAs (miRNAs).
in vitro: GEN effectively reversed estrogenicity of BPA by reversing mRNA and protein expressions of ERα, IGF-1R, pIRS-1, and pAkt induced by BPA in cellular model and also significantly decreased tumor growth and in vivo expressions of ERα, pIRS-1, and pAkt in xenografted mouse model [1]. Interestingly, genistein and its analogs induced caspase 3-activation supporting apoptotic mechanism of cell death but SPG-G supported caspase 3-independent apoptosis [2]. Of the compounds tested, only genistein selectively inhibited human topo II activity and had an IC50 value of 37.5 ?M [3]
in vivo: Genistein significantly decreased the blood levels of total cholesterol, triglycerides, homocysteine and visfatin compared with placebo, while blood adiponectin levels were increased [4]. Leucine and genistein significantly (p<0.05) reduced the number of fights and increased latency to fights in foot shock-induced aggression; it also decreased apomorphine (5mg/kg, i.p.) induced stereotyped behavior and apomorphine induced (10mg/kg, s.c.) locomotor activity when compared with the positive control group [5].
Clinical trial: Cholecalciferol and Genistein Before Surgery in Treating Patients With Early Stage Prostate Cancer. Phase 2
 .Phytoestrogen found in soy beans. Anticancer agent. Inihibits tyrosine protein kinase and DNA topoisomerase as well as possessing antioxidant and cell cycle inhibitor activity. Endocytosis inhibitor.
应用 1、具有雌性激素及抗雌激素性质 2、在体内能抑制结肠癌、乳腺癌、皮肤癌、前列腺癌等 3、对多种肿瘤细胞株有抑制作用 4、具有抗氧化作用 5、可以抑制酪氨酸蛋白激酶(PTK)的活性 6、可以抑制拓扑异购酶Ⅱ的活性 7、可以预防绝经后骨质疏松 8、具有诱发细胞程序性死亡、提高抗癌药效、抑制血管生成等作用,是一种很有潜力的癌症化学预防剂,其抗癌作用及机制具有广泛的应用前景。
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 如果有可能,您尽量在使用的当天配置溶液,并在当天使用完它。但是,如果您需要预先配制储备溶液,我们建议您将溶液等份保存在-20°C的密封小瓶中。通常,它们最多可以使用一个月。在使用前和打开样品瓶之前,我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。
产品介绍

溶于乙醇和DMSO, 干冷处保存。

名称和标识符

PubChem SID 488195220
EC号 207-174-9
IUPAC Name 5,7-dihydroxy-3-(4-hydroxyphenyl)chromen-4-one
INCHI InChI=1S/C15H10O5/c16-9-3-1-8(2-4-9)11-7-20-13-6-10(17)5-12(18)14(13)15(11)19/h1-7,16-18H
InChi Key TZBJGXHYKVUXJN-UHFFFAOYSA-N
Canonical SMILES C1=CC(=CC=C1C2=COC3=CC(=CC(=C3C2=O)O)O)O
Isomeric SMILES C1=CC(=CC=C1C2=COC3=CC(=CC(=C3C2=O)O)O)O
WGK Germany 3
RTECS NR2392000
PubChem CID 5280961
分子量 270.24
Beilstein号 263823
Reaxy-Rn 263823

化学和物理性质

密度 1.548
敏感性 对热敏感
熔点 297-298°C

安全和危险性(GHS)

象形图
ghs09

Environmental Hazard

ghs07

Harmful

信号词 Warning
危险声明 H315: Causes skin irritation
H319: Causes serious eye irritation
H335: May cause respiratory irritation
H302: Harmful if swallowed
H400: Very toxic to aquatic life
H410: Very toxic to aquatic life with long lasting effects
预防措施声明 P261,P305+P351+P338,P273,P280,P302+P352,P321,P405,P501,P264,P271,P270,P304+P340,P403+P233,P362+P364,P391,P330,P264+P265,P301+P317,P337+P317,P332+P317,P319
WGK Germany 3
RTECS NR2392000
Reaxy-Rn 263823
Merck Index 4391
个人防护装备 Eyeshields,Faceshields,Gloves,type N95 (US),type P1 (EN143) respirator filter

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质检报告(COA)

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参考文献

1. Hamouda NN, Van den Haute C, Vanhoutte R, Sannerud R, Azfar M, Mayer R, Cortés Calabuig Á, Swinnen JV, Agostinis P, Baekelandt V et al..  (2020)  ATP13A3 is a major component of the enigmatic mammalian polyamine transport system..  J Biol Chem,  71  (13):  (1755-70).  [PMID:33310703]
2. van Veen S et al..  (2020)  ATP13A2 deficiency disrupts lysosomal polyamine export..  Nature,  578  (7795):  (419-424).  [PMID:31996848]
3. Piepgras J et al..  (2022)  Enhancement of Phosphorylation and Transport Activity of the Neuronal Glutamate Transporter Excitatory Amino Acid Transporter 3 by C3bot and a 26mer C3bot Peptide..  Front Cell Neurosci,  16  ():  (860823).  [PMID:35783090]
4. Martin-Gallausiaux C et al..  (2020)  Fusobacterium nucleatum Extracellular Vesicles Modulate Gut Epithelial Cell Innate Immunity via FomA and TLR2..  Front Immunol,  11  ():  (583644).  [PMID:33408714]
5. Jayagopal A et al..  (2010)  Hairpin DNA-functionalized gold colloids for the imaging of mRNA in live cells..  J Am Chem Soc,  132  (28):  (9789-96).  [PMID:20586450]
6. Sobhy MMK et al..  (2018)  Impact of treatment with a Protein Tyrosine Kinase Inhibitor (Genistein) on acute and chronic experimental Schistosoma mansoni infection..  Exp Parasitol,  185  ():  (115-123).  [PMID:29331278]
7. Ardito F et al..  (2017)  In vitro study on anti-cancer properties of genistein in tongue cancer..  Onco Targets Ther,  10  ():  (5405-5415).  [PMID:29180873]
8. Valeri A et al..  (2012)  The soy phytoestrogens genistein and daidzein as neuroprotective agents against anoxia-glucopenia and reperfusion damage in rat urinary bladder..  Pharmacol Res,  66  (4):  (309-16).  [PMID:22743170]