1. Metabolic Enzyme/Protease PI3K/Akt/mTOR Epigenetics
  2. Oxidative Phosphorylation Mitochondrial Metabolism AMPK
  3. AMPK activator 11

AMPK activator 11 是一种 AMP 活化蛋白激酶激活因子,具有纳米水平的抗肿瘤活性,可以抵抗多种 CRC。AMPK activator 11 通过激活 AMPK 和上调氧化磷酸化 (OXPHOS) ( mitochondrial metabolism ) 选择性地抑制 RKO 异种移植物的生长,可用于抗肿瘤及代谢性疾病研究。

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AMPK activator 11 Chemical Structure

AMPK activator 11 Chemical Structure

CAS No. : 2948304-00-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AMPK activator 11 is an AMP-activated protein kinase (AMPK) activator with nanomolelevel antiproliferation activities against several CRCs. AMPK activator 11 selectively inhibits the RKO xenograft growth along by activating AMPK and upregulating oxidative phosphorylation (OXPHOS) ( mitochondrial metabolism ) and can be used for anti-tumor and metabolic disease research[1].

体外研究
(In Vitro)

AMPK activator 11 (Compound 18a) (0-30 μM;0-7 天) 抑制 CRC 细胞的生长和迁移,对其 IC50 值低于 1 μM[1]
AMPK activator 11 (0-0.1 μM;24 小时) 显著提高 RKO 细胞的全局耗氧率 (OCR) ,同时细胞外酸化率 (ECAR) 轻微变化。AMPK activator 11 上调 p-AMPK 和线粒体复合物 III 和 V 的表达,并且具有在 CRC 中选择性激活 OXPHOS 的能力[1]

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

Cell Viability Assay[1]

Cell Line: CRC cells
Concentration: 0-30 μM
Incubation Time: 0-7 days
Result: Selectively inhibited the growth and migration of CRC cells.
Inhibited the proliferation of different CRCs with IC50 values below 1 μM.

Western Blot Analysis[1]

Cell Line: RKO cells
Concentration: 0.1 μM
Incubation Time: 24 hours
Result: Upregulated the expression of p-AMPK and mitochondrial complex III and V and has the ability to selectively activate OXPHOS.
体内研究
(In Vivo)

AMPK activator 11 (Compound 18a) (2.5 或 10 mg/kg 腹腔注射,持续 25 天) 选择性抑制 RKO 细胞体外异种肿瘤模型的肿瘤生长,且无毒性[1]>。

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

Animal Model: RKO cells related axenograft model on male BALB/nude mice[1]
Dosage: 2.5 or 10 mg/kg
Administration: Intraperitoneal injection (i.p.) for 25 days
Result: Resulted in 58.2% tumor growth inhibition, with no significant weight loss observed.
Resulted in 77.1% inhibition of tumor growth but also caused a 36% weight loss.
Immunohistochemistry results also showed activation of AMPK in tumor tissue.
分子量

408.45

Formula

C25H20N4O2

CAS 号
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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  • 稀释计算器

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Help & FAQs
  • 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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产品名称:
AMPK activator 11
目录号:
HY-154973
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