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概述
AP-III-a4 (ENOblock) hydrochloride is a nonsubstrate analogue enolase inhibitor with an IC 50 of 0.576 uM. AP-III-a4 hydrochloride can be used for the research of cancer and diabetic
In Vitro
AP-III-a4 (ENOblock) (0-10 μM; 24 h) inhibits HCT116 cell viability in a dose-dependent manner. AP-III-a4 directly binds to enolase and inhibits its activity. AP-III-a4 (0-10 μM; 24 or 48 h) inhibits cancer cell migration and invasion, induces cancer cell apoptosis. AP-III-a4 (10 μM; 24 h) can induce glucose uptake and inhibit phosphoenolpyruvate carboxykinase (PEPCK) expression in hepatocytes and kidney cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: HCT116 Concentration: 1.25, 2.5, 5 and 10 μM Incubation Time: 24 h Result: Induced higher levels of HCT116 colon cancer cell death in hypoxic conditions compared to normoxia. Western Blot AnalysisCell Line: HCT116 Concentration: 1.25, 2.5, 5 and 10 μM Incubation Time: 24 h for AKT, 48 h for Bcl-Xl Result: Bound to enolase in cell lysate and bound to purified enolase. Decreased the expression of AKT and Bcl-Xl, which are negative regulators of apoptosis. Cell Invasion AssayCell Line: HCT116 Concentration: 0.156, 0.312, 0.625, 1.25 and 2.5 μM Incubation Time: 24 h Result: Significantly inhibits cancer cell invasion at a treatment concentration of 0.625 μM. Cell Migration AssayCell Line: HCT116 Concentration: 0.625, 1.25 and 2.5 μM Incubation Time: 24 h Result: Inhibited cell migration dose-dependently. RT-PCRCell Line: Huh7 and HEK Concentration: 10 μM Incubation Time: 24 h Result: Induced glucose uptake and inhibited PEPCK expression.
In Vivo
AP-III-a4 (ENOblock) (10 μM; 96 h) inhibits cancer cell metastasis and suppresses the gluconeogenesis regulator PEPCK in zebrafish . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: The zebrafish cancer cell HCT116 xenograft model Dosage: 10 μM Administration: 96 h Result: Reduced cancer cell dissemination. Inhibited PEPCK expression and induced glucose uptake. Inhibited adipogenesis and foam cell formation.
Form:Solid
IC50& Target:IC 50 : 0.576 uM (enolase)
规格
别名
AP-III-a4盐酸盐
规格或纯度
≥98%
英文名称
AP-III-a4 hydrochloride
生化机理
AP-III-a4 (ENOblock) 盐酸盐是一种非底物类似物烯醇化酶抑制剂，IC 50 为 0.576 uM。AP-III-a4 盐酸盐可用于癌症和糖尿病的研究。
储存条件
2-8°C储存,干燥
运输条件
低温运输
作用类型
抑制剂
纯度
≥98%
名称和识别符
分子类型
小分子
分子量
631.18
高级数据
化学和物理性质
溶解性
DMSO : ≥ 53 mg/mL (83.97 mM) H2O : <0.1 mg/mL (insoluble)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
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