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N-(2-(2-(2-氨基乙氧基)乙氧基)乙基)-2-(4-((4-((环己基甲基)氨基)-6-((4-氟苄基)氨基)-1,3,5-三嗪-2-基)氨基)苯基)乙酰胺

更新时间:2024-07-15 12:30:25 采购访问:13次

常用名 AP-III-A4 CAS号 1177827-73-4
价格 纯度 98.0%
备货期 10天 库存 现货
 产品详情(用途,包装等)
用途:
ENOblock(AP-III-a4) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.IC50 value: 0.576 uM [1]Target: enolaseEnolase is a component of the glycolysis pathway and a “moonlighting” protein, with important roles in diverse cellular processes that are not related to its function in glycolysis. However, small molecule tools to probe enolase function have been restricted to crystallography or enzymology. In this study, we report the discovery of the small molecule “ENOblock”, which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity. ENOblock was isolated by small molecule screening in a cancer cell assay to detect cytotoxic agents that function in hypoxic conditions, which has previously been shown to induce drug resistance. Further analysis revealed that ENOblock can inhibit cancer cell metastasis in vivo. Moreover, an unexpected role for enolase in glucose homeostasis was revealed by in vivo analysis. Thus, ENOblock is the first reported enolase inhibitor that is suitable for biological assays. This new chemical tool may also be suitable for further study as a cancer and diabetes drug candidate.A Unique Small Molecule Inhibitor of Enolase Clarifies Its Role in Fundamental Biological ProcessesBy Jung, Da-Woon; Kim, Woong-Hee; Park, Si-Hwan; Lee, Jinho; Kim, Jinmi; Su, Dongdong; Ha, Hyung-Ho; Chang, Young-Tae; Williams, Darren R. From ACS Chemical Biology (2013), 8(6), 1271-1282.
物理化学性质:
CAS号:1177827-73-4
常用中文名:AP-III-A4
常用英文名:AP-III-a4
分子式:C31H43FN8O3
分子量:594.723
密度:1.3±0.1 g/cm3
沸点:N/A
熔点:N/A
闪点:N/A
储存条件:-20℃

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参考价格:$288/5mg