Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AP-III-a4 (ENOblock) 是第一个非底物类似物,可直接与烯醇酶结合,IC50=0.576 uM,可阻碍体内癌细胞转移。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 497 | 现货 | ||
5 mg | ¥ 1,690 | 现货 | ||
10 mg | ¥ 2,750 | 现货 | ||
25 mg | ¥ 4,590 | 现货 | ||
50 mg | ¥ 6,550 | 现货 | ||
100 mg | ¥ 8,930 | 现货 |
产品描述 | AP-III-a4 (ENOblock) (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 μM. |
靶点活性 | Enolase:0.576 μM |
体外活性 | AP-III-a4 induces glucose uptake and inhibits phosphoenolpyruvate carboxykinase (PEPCK) expression in Huh7 hepatocytes and HEK kidney cells. AP-III-a4 induces cell death under hypoxia, and inhibits cancer cell migration and invasion by down-regulation of AKT and Bcl-xL expression in HCT116 cells. |
体内活性 | AP-III-a4 (10 μM) inhibits cancer cell migration and invasion processes in HCT116-xenotransplanted zebrafish tumor model. In vivo, AP-III-a4 (10 μM) also inhibits adipogenesis and foam cell formation, and causes downregulation of PEPCK expression and induction of glucose uptake. |
激酶实验 | Enolase activity assay is in the 2.0 mM MgSO4 and 400 mM KCl in the absence or presence of ENOblock or NaF, at 37°C by incubating pure enolase (3–9 U) in a buffer containing 50 mM imidazole-HCl (pH 6.8). The reaction is initiated by adding 1 μmol of 2-phospho-D-glycerate, and the OD is measured after 10 min of reaction time with a spectrophometer at 240 nm. |
细胞实验 | HCT116 cells(3 x 10E5) are seeded in a 6 well plate. 24 h later, cells are treated with AP-III-a4 (5 μM) for 24hours. |
动物实验 | In HCT116-xenotransplanted zebrafish tumor xenograft model, were treated with AP-III-a4 of 10 μM. |
别名 | ENOblock |
分子量 | 594.72 |
分子式 | C31H43FN8O3 |
CAS No. | 1177827-73-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL (47.53 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.6815 mL | 8.4073 mL | 16.8146 mL | 42.0366 mL |
5 mM | 0.3363 mL | 1.6815 mL | 3.3629 mL | 8.4073 mL | |
10 mM | 0.1681 mL | 0.8407 mL | 1.6815 mL | 4.2037 mL | |
20 mM | 0.0841 mL | 0.4204 mL | 0.8407 mL | 2.1018 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AP-III-a4 1177827-73-4 Metabolism Glucokinase Inhibitor AP-III-a-4 Phosphopyruvate hydratase Apoptosis inhibit antidiabetic anticancer HCT116 Enolase Huh7 zebrafish APIIIa4 ENOblock HEK AP III a4 inhibitor