AP-III-a4 (ENOblock) hydrochloride 是一种非底物类似物烯醇酶 (enolase) 抑制剂，IC50为 0.576 uM。 AP-III-a4 hydrochloride 可用于癌症和糖尿病研究。
| 生物活性 | AP-III-a4 (ENOblock) hydrochloride is a nonsubstrate analogueenolaseinhibitor with anIC50of 0.576 uM. AP-III-a4 hydrochloride can be used for the research ofcancerand diabetic[1]. |
| IC50& Target | IC50: 0.576 uM (enolase)[1] |
体外研究
(In Vitro) | AP-III-a4 (ENOblock) (0-10 μM; 24 h) inhibits HCT116 cell viability in a dose-dependent manner[1].
AP-III-a4 directly binds to enolase and inhibits its activity[1].
AP-III-a4 (0-10 μM; 24 or 48 h) inhibits cancer cell migration and invasion, induces cancer cell apoptosis[1].
AP-III-a4 (10 μM; 24 h) can induce glucose uptake and inhibit phosphoenolpyruvate carboxykinase (PEPCK) expression in hepatocytes and kidney cells[1].
Cell Viability Assay[1] | Cell 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 Analysis[1] | Cell 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 Assay[1] | Cell 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 Assay[1] | Cell Line: | HCT116 | | Concentration: | 0.625, 1.25 and 2.5 μM | | Incubation Time: | 24 h | | Result: | Inhibited cell migration dose-dependently. |
RT-PCR[1] | Cell Line: | Huh7 and HEK | | Concentration: | 10 μM | | Incubation Time: | 24 h | | Result: | Induced glucose uptake and inhibited PEPCK expression. |
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体内研究
(In Vivo) | AP-III-a4 (ENOblock) (10 μM; 96 h) inhibits cancer cell metastasis and suppresses the gluconeogenesis regulator PEPCK in zebrafish[1].
| Animal Model: | The zebrafish cancer cell HCT116 xenograft model[1] | | Dosage: | 10 μM | | Administration: | 96 h | | Result: | Reduced cancer cell dissemination. Inhibited PEPCK expression and induced glucose uptake. Inhibited adipogenesis and foam cell formation. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : ≥ 53 mg/mL(83.97 mM) H2O :< 0.1 mg/mL(insoluble) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 1.5843 mL | 7.9217 mL | 15.8433 mL | | 5 mM | 0.3169 mL | 1.5843 mL | 3.1687 mL | | 10 mM | 0.1584 mL | 0.7922 mL | 1.5843 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.30 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.30 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.30 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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