A-769662
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mL(10 mM in DMSO) | ￥636.00 | 现货 | |
| 10mg | ￥590.00 | 现货 | |
| 25mg | ￥1272.00 | 现货 | |
| 50mg | ￥2363.00 | 现货 |
特色产品
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 对细胞无毒性
- 步骤更简单，无需有机溶剂
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量
产品描述
A-769662是一种有效的AMPK激活剂，在体外的EC50值为0.8μM[1]。
AMP激活蛋白激酶（AMPK）是一种丝氨酸/苏氨酸蛋白激酶，由三种亚基形成：α、β和γ亚基，它们在AMPK的活性和稳定性方面具有重要作用。 AMPK作为细胞能量的传感器，检测和反应AMP: ATP比值的变化。AMPK在调控细胞内能量代谢方面具有重要作用。AMPK抑制ATP消耗通路，包括胆固醇合成、脂肪酸合成和糖异生。AMPK刺激产生ATP的脂肪酸氧化和糖酵解过程。AMPK通过抑制葡萄糖-6-磷酸酶和PEPCK的表达（两个关键的糖异生酶），从而抑制糖异生[1]。
A-769662属于thienopyridone家族，以剂量依赖的方式激活不同组织来源的纯化AMPK的活性。A-769662激活从人胚胎肾细胞（HEKs）、大鼠肌肉或大鼠心脏提取的AMPK活性，EC50值分别为1.1 mM、1.9 mM或2.2 mM。在原代大鼠肝细胞中，A-769662抑制脂肪酸的合成，IC50值为3.2 mM [1]。A769662也以AMPK不依赖的机制抑制26S蛋白酶体，从而引起细胞周期停滞，而不抑制20S核心亚基的蛋白水解活性[2]。A-769662以变构的方式激活AMPK，也抑制AMPK的Thr-172去磷酸化[3]。
在小鼠中，A-769662以30 mg/kg的剂量给药后减少肝脏中FAS、G6Pase和PEPCK的表达，也降低了40%的血浆葡萄糖水平，并减少体重的增加[1]。
参考文献：
[1]. Cool B, Zinker B, Chiou W, Kifle L, Cao N, Perham M, Dickinson R, Adler A, Gagne G, Iyengar R et al: Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome. Cell Metab 2006, 3(6):403-416.
[2]. Moreno D, Knecht E, Viollet B, Sanz P: A769662, a novel activator of AMP-activated protein kinase, inhibits non-proteolytic components of the 26S proteasome by an AMPK-independent mechanism. FEBS Lett 2008, 582(17):2650-2654.
[3]. Sanders MJ, Ali ZS, Hegarty BD, Heath R, Snowden MA, Carling D: Defining the mechanism of activation of AMP-activated protein kinase by the small molecule A-769662, a member of the thienopyridone family. J Biol Chem 2007, 282(45):32539-32548.
产品性质
| 物理外观 | A solid |
| CAS号 | 844499-71-4 |
| 分子式 | C20H12N2O3S |
| 分子量 | 360.39 |
| 化学名称 | 4-hydroxy-3-[4-(2-hydroxyphenyl)phenyl]-6-oxo-7H-thieno[2,3-b]pyridine-5-carbonitrile |
| 溶解度 | insoluble in EtOH; insoluble in H2O; ≥18.02 mg/mL in DMSO |
| SMILES | N#CC(C(Nc1c2c(-c(cc3)ccc3-c(cccc3)c3O)c[s]1)=O)=C2O |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)
IC50和靶点
| 生物活性描述 | A-769662是AMPK的小分子激活剂，IC50值为116 nM。 |
| 靶点 | AMPK |
| 生物活性数据 | 116 nM (EC50) |
生物相关数据
质量控制
APExBIO 顾客使用本产品发表的 9 篇科研文献
- 1. Ji-Man Park, Da-Hye Lee, et al. "Redefining the role of AMPK in autophagy and the energy stress response." Nat Commun. 2023 May 24;14(1):2994. PMID: 37225695
- 2. Pier, Marissa. "AMP-Activated Protein Kinase (AMPK) and Estrogen-Dependent Mechanisms Underlying Increased Susceptibility to Cardiovascular Disease During Menopause." The University of Arizona.
- 3. Yong Heui Jeon, Minzhen He, et al. "Adiponectin enhances the bioenergetics of cardiac myocytes via an AMPK-and succinate dehydrogenase-dependent mechanism." Cell Signal. 2021 Feb;78:109866. PMID: 33271223
- 4. Tereza Moore, Rolando E. Yanes, et al. "AMP-independent activator of AMPK for treatment of mitochondrial disorders." PLoS One. 2020 Oct 14;15(10):e0240517. PMID: 33052980
- 5. Matzinger M, Fischhuber K, et al. "AMPK leads to phosphorylation of the transcription factor Nrf2, tuning transactivation of selected target genes." Redox Biol. 2019 Nov 27;29:101393. PMID: 31805502
- 6. Cannon, Danielle Kathryn. "ASSESSING MENOPAUSAL FEMALE SUSCEPTIBILITY TO HEART DISEASE: A FOCUS ON AMPK’S ABILITY TO MITIGATE CARDIAC REMODELING THROUGH ESTROGEN-DEPENDENT GENE PROGRAMS." The University of Arizona. 2019.
- 7. Wen Z, Jin K, et al. "N-myristoyltransferase deficiency impairs activation of kinase AMPK and promotes synovial tissue inflammation." Nat Immunol. 2019 Mar;20(3):313-325. PMID: 30718913
- 8. Hubbard JA, Xiao B, et al. "Production and Crystallization of Full-Length Human AMP-Activated Protein Kinase (α1β1γ1)." Methods Mol Biol. 2018;1732:1-14. PMID: 29480465
- 9. Oladimeji PO, Lin W, et al. "Glucose-dependent regulation of pregnane X receptor is modulated by AMP-activated protein kinase." Sci Rep. 2017 Apr 24;7:46751. PMID: 28436464
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