| Bioactivity | 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]. |
| Invitro | 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]。 Cell Viability Assay[1] Cell Line: |
| 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]>。 Animal Model: |
| Name | AMPK activator 11 |
| Formula | C25H20N4O2 |
| Molar Mass | 408.45 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Xu YH,et.al. Design and Synthesis of Bouchardatine Derivatives as a Novel AMP-Activated Protein Kinase Activator for the Treatment of Colorectal Cancer. J Med Chem. 2023 Jun 8;66(11):7387-7404. |