ENOblock is a small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 μM) and inhibit cancer cell metastasis in vivo.
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描述 | AP-III-a4 is a novel nonsubstrate analogue inhibitor of enolase, exhibiting an IC50 of 0.576 μM, making it relevant for cancer and diabetes research[1]. |
体内研究 | Moreover, at the concentration of 10 μM over 96 hours, AP-III-a4 hinders cancer cell metastasis and downregulates PEPCK in zebrafish, indicating its efficacy against cancer cell spread and its impact on gluconeogenesis[1]. |
体外研究 | AP-III-a4 demonstrates a dose-dependent inhibition of HCT116 cell viability over 24 hours when used in concentrations ranging from 0 to 10 μM, that also impairs cancer cell migration and invasion[1]. Notably, AP-III-a4 induces glucose uptake and reduces the expression of phosphoenolpyruvate carboxykinase (PEPCK) in hepatocytes and kidney cells when applied at 10 μM for 24 hours, suggesting potential benefits for managing diabetic conditions[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.68mL 0.34mL 0.17mL |
8.41mL 1.68mL 0.84mL |
16.81mL 3.36mL 1.68mL |
CAS号 | 1177827-73-4 |
分子式 | C31H43FN8O3 |
分子量 | 594.723 |
别名 | ENOblock |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,2-8°C |
溶解度 |
DMSO: 105 mg/mL(176.55 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |