1. Apoptosis
  2. Apoptosis Caspase
  3. 4′-O-Methylglabridin

4′-O-Methylglabridin  (Synonyms: 4′-O-甲基光甘草定)

目录号: HY-N11846
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4′-O-Methylglabridin 是一种凋亡 (apoptosis) 诱导剂,具有抗氧化、细胞周期干扰及抗癌细胞毒活性。4′-O-Methylglabridin 可抑制肝癌、乳腺癌和结直肠癌等多种癌细胞系。4′-O-Methylglabridin 通过降低磷酸化 Rb (Ser807/811) p21 蛋白的表达水平,促使细胞在 subG1 和 G2/M 期累积,并经由细胞色素 C 释放及 Caspase-9 活化触发 Caspase 依赖性凋亡。4′-O-Methylglabridin 还能通过抑制脂质过氧化物水平和减少 β-胡萝卜素消耗来发挥抗氧化作用,从而阻断 LDL 氧化。4′-O-Methylglabridin 可用于多种癌症及动脉粥样硬化疾病研究。

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4′-O-Methylglabridin

4′-O-Methylglabridin Chemical Structure

CAS No. : 68978-09-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

4′-O-Methylglabridin is an apoptosis inducer with antioxidant, cell cycle-disrupting and anticancer cytotoxic activities. 4′-O-Methylglabridin inhibits various cancer cell lines including liver cancer, breast cancer and colorectal cancer cell lines. By reducing the expression levels of phosphorylated Rb (Ser807/811) and p21 proteins, 4′-O-Methylglabridin promotes cell accumulation at the subG1 and G2/M phases, and triggers caspase-dependent apoptosis via cytochrome C release and caspase-9 activation. 4′-O-Methylglabridin also exerts antioxidant effects by inhibiting lipid peroxide levels and reducing β-carotene consumption, thereby blocking LDL oxidation. 4′-O-Methylglabridin can be used in the research of various cancers and atherosclerotic diseases[1][2].

IC50 & Target[1]

Caspase-9

 

体外研究
(In Vitro)

4′-O-Methylglabridin (2.5-40 μM; 72 h) 可在体外抑制 Huh7、MCF7 和 HCT116 癌细胞系的增殖,其中对 Huh7 细胞的活性最强 (IC50=9.6 μM)[1]
4′-O-Methylglabridin (IC50; 24 h, 48 h, 72 h) 可呈时间依赖性抑制 Huh7 细胞增殖,其 IC50 值从 24 h 时的 7.31 μM 升高至 72 h 时的 11.4 μM[1]
4′-O-Methylglabridin (10 μM; 48 h) 处理 Huh7 细胞 48 h 后可诱导其出现凋亡性细胞核变化,该过程中,检测到 subG1 期积累及 G2/M 期阻滞[1]
4′-O-Methylglabridin (10 μM; 48 h) 可通过增加细胞色素 C 的释放和活化型 caspase-9 的水平,诱导 Huh7 细胞发生 caspase 依赖性凋亡,同时还会降低磷酸化 Rb、p53、Mdm2 和 p21 的水平以破坏细胞周期调控[1]
4′-O-Methylglabridin (50 μM; 90 min; 50°C) 在无细胞 β-胡萝卜素-亚油酸分析中可抑制 78%的 β-胡萝卜素消耗[2]
4′-O-Methylglabridin (30 μM; 2 h; 37°C) 可强效抑制 AAPH 诱导的体外 人 LDL 氧化[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: Huh7, MCF7, HCT116
Concentration: 2.5, 5, 10, 20, 40 μM
Incubation Time: 72 h
Result: Inhibited proliferation of Huh7 cells with an IC50 of 9.6 μM.
Inhibited proliferation of MCF7 cells with an IC50 of 16.5 μM.
Inhibited proliferation of HCT116 cells with an IC50 of 10.8 μM.

Cell Proliferation Assay[1]

Cell Line: Huh7
Concentration: IC50 concentration Test
Incubation Time: 24 h, 48 h, 72 h (monitored every 10 min for first 24 h, then every 30 min for remaining 48 h)
Result: Inhibited Huh7 cell proliferation with an IC50 of 7.31 μM at 24 h.
Inhibited Huh7 cell proliferation with an IC50 of 9.8 μM at 48 h.
Inhibited Huh7 cell proliferation with an IC50 of 11.4 μM at 72 h.

Apoptosis Analysis[1]

Cell Line: Huh7
Concentration: 10 μM
Incubation Time: 48 h
Result: Increased the percentage of Huh7 cells in the subG1 phase to 5.26% relative to DMSO control.
Induced accumulation of Huh7 cells in the G2/M phase to 20.32% relative to DMSO control.
Induced changes in Huh7 cell nuclei consistent with apoptotic cell death, as detected by Hoechst staining.

Western Blot Analysis[1]

Cell Line: Huh7
Concentration: 10 μM (48 h IC50)
Incubation Time: 48 h
Result: Increased cytochrome C and cleaved caspase-9 protein levels relative to DMSO control.
Decreased phospho-Rb (Ser807/811), p53, Mdm2, and p21 protein levels relative to DMSO control.
Did not increase cleaved PARP protein levels relative to DMSO control.
分子量

338.40

Formula

C21H22O4

CAS 号
中文名称

4′-O-甲基光甘草定

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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4′-O-Methylglabridin
目录号:
HY-N11846
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