染料木素 T1737

Product Introduction
Bioactivity


英文名: Genistein

描述: Genistein (NPI 031L) 是一种大豆异黄酮，是一种多重的酪氨酸激酶抑制剂，通过改变细胞凋亡，细胞周期和血管生成以及抑制转移对多种癌症有化疗作用。

细胞实验: Genistein is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. The IC50 values for Genistein are determined by the MTT assay. Briefly, the MTT assay is a colorimetric assay that is based on the ability of living but not dead cells to reduce a tetrazolium-based compound to a blue formazan product. The formazan crystals are solubilized in DMSO, and the absorbance is measured at 540 nm. The absorbance at 540 nm is proportional to the number of viable cells. The lC50 values obtained with the MTT assay are compared with the lC50 values obtained by counting viable cells using trypan blue dye exclusion and by tritiated thymidine incorporation into DNA[1].

激酶实验: Purified FXa is obtained after activation with Russell's viper venom followed by affinity chromatography. The resulting FXa is > 95% pure as judged by sodium dodecylsulfate polyacrylamide gel electrophoresis. The substrate affinity values for FXa, expressed as the Michaelis-Menten-Henri constant (Km), for human, rabbit, rat and dog FXa are determined using the chromogenic substrate S-2765, and are 36, 60, 240 and 70 μM, respectively. The substrate hydrolysis is monitored by measuring absorbance at 405 nm at 25°C for up to 30 min using a SpectraMax 384 Plus plate reader and SoftMax. FXa activity for each substrate and inhibitor concentration pair is determined in duplicate. The Ki values are calculated by non-linear least-squares fitting of the steady-state substrate hydrolysis rates to the equation for competitive inhibition (Equation 1) using GRAFIT, where v equals reactions velocity in OD min?1, Vmax equals maxiumum reaction velocity, S equals substrate concentration, and I equals inhibitor concentration.

体外活性: 对于成年动物的乳腺癌,前列腺癌和其它内分泌依赖性肿瘤,Genistein具有预防作用.在小鼠中,Genistein与前列腺肿瘤辐射结合,能够抑制原发性肿瘤的生长,控制肿瘤细胞向主动脉旁淋巴结的转移.

体内活性: Genistein作为GPR30受体的激动剂,能够与PPARγ结合（Ki=5.7 μM）。在A431表皮癌细胞中,Genistein抑制EGF刺激的酪氨酸磷酸化。在NIH-3T3细胞中,Genistein阻断EGF,胰岛素和凝血酶介导的促有丝分裂作用。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (166.52 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 2 mg/mL (7.4 mM)


关键字: EGFR | HER1 | ErbB-1 | Endogenous Metabolite | Apoptosis | Autophagy | Inhibitor | Epidermal growth factor receptor | Genistein | inhibit

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相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Tobacco Monomer Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Traditional Chinese Medicine Monomer Library | Anti-Cancer Active Compound Library | Miao medicine Compound Library | Antiparasitic Natural Product Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途