Desmethylglycitein(Synonyms: 4′,6,7-三羟基异黄酮; 4′,6,7-Trihydroxyisoflavone)

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Desmethylglycitein (Synonyms: 4′,6,7-三羟基异黄酮; 4′,6,7-Trihydroxyisoflavone) 纯度: ≥95.0%

Desmethylglycitein (4′,6,7-Trihydroxyisoflavone),大豆苷元的代谢产物,来源于大豆 Glycine max,具有抗氧化性和抗癌活性。Desmethylglycitein 在体内直接结合 CDK1CDK2,抑制 CDK1 和 CDK2 活性。Desmethylglycitein 是蛋白激酶 C (PKC)α 的直接抑制剂,抑制正常人皮肤成纤维细胞中的太阳紫外线 (sUV) 诱导的基质金属蛋白酶1 (MMP1)。Desmethylglycitein 以 ATP 竞争方式与细胞质中的 PI3K 结合,抑制 PI3K 和下游信号级联的活性,从而抑制 3T3-L1 前脂肪细胞中的脂肪形成。

Desmethylglycitein(Synonyms: 4

Desmethylglycitein Chemical Structure

CAS No. : 17817-31-1

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Desmethylglycitein 相关产品

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  • Bioactive Compound Library Plus

生物活性

Desmethylglycitein (4′,6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity[1]. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1)[2]. Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes[3].

IC50 & Target[1][2][3]

CDK1

 

CDK2

 

PKC

 

体外研究
(In Vitro)

Desmethylglycitein (4′,6,7-Trihydroxyisoflavone)(0-100 μM; 24-72 hours) suppesses anchorage-dependent growth of HCT-116 and DLD1 cells in a dose- and time-dependent manner without cytotoxicity [1].
Desmethylglycitein (4′,6,7-Trihydroxyisoflavone)(0-100 μM; 24-72 hours) suppresses CDK1 activity in a dose-dependent manner and inhibits CDK2 activity in HCT-116 cells[1].
Desmethylglycitein (4′,6,7-Trihydroxyisoflavone)(0-100 μM; 24-72 hours) induces cell cycle arrest at the S and G2/M phases, the percentage of cells in S phase is higher in the 100 μM 6,7,4′-THIF-treated group, and the same pattern is observed in G2/M phase (29.5% versus 19.1% ) [1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HCT-116 cells
Concentration: 0, 12.5, 25, 50 or 100 μM
Incubation Time: 24, 48 or 72 hours
Result: Inhibited anchorage-dependent and -independent growth of HCT-116 cells.

Western Blot Analysis[1]

Cell Line: HCT-116 and DLD1 cells
Concentration: 0, 25, 50 or 100 μM
Incubation Time: 48 hours
Result: Inhibited CDK1,CDK2 expression.

Cell Cycle Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0, 25, 50 or 100 μM
Incubation Time: 24, 48 or 72 hours
Result: Induces cell cycle arrest of HCT-116 cells at S and G2/M phases.

体内研究
(In Vivo)

Desmethylglycitein (4′,6,7-Trihydroxyisoflavone) (intraperitoneally injection; 5 or 25 mg/kg; once daily; 20 days) suppresses tumor development in mice and serves as an effective anticancer treatment with the potential to inhibit or delay the tumorigenicity of HCT-116 cells in an in vivo system[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nude mice subcutaneously injected with HCT-116 cells[1]
Dosage: 5 or 25 mg/kg
Administration: Intraperitoneally injection; 5 or 25 mg/kg; once daily; 20 days
Result: Decreased tumor growth, volume and weight of HCT-116 xenografts.

分子量

270.24

Formula

C15H10O5

CAS 号

17817-31-1

中文名称

4′,6,7-三羟基异黄酮

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (462.55 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7004 mL 18.5021 mL 37.0041 mL
5 mM 0.7401 mL 3.7004 mL 7.4008 mL
10 mM 0.3700 mL 1.8502 mL 3.7004 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.70 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.70 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.70 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.70 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.70 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.70 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Lee DE, et al. 6,7,4′-trihydroxyisoflavone inhibits HCT-116 human colon cancer cell proliferation by targeting CDK1 and CDK2. Carcinogenesis. 2011 Apr;32(4):629-35.

    [2]. Lim TG, et al. The daidzein metabolite, 6,7,4′-Trihydroxyisoflavone, is a novel inhibitor of PKCα in suppressing solar UV-induced matrix metalloproteinase 1. Int J Mol Sci. 2014 Nov 19;15(11):21419-32

    [3]. Seo SG, et al. A metabolite of daidzein, 6,7,4′-trihydroxyisoflavone, suppresses adipogenesis in 3T3-L1 preadipocytes via ATP-competitive inhibition of PI3K.

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