AP-III-a4 hydrochloride ENOblock hydrochloride|cas:2070014-95-6|西域试剂

AP-III-a4 hydrochloride ENOblock hydrochloride,98.96%

产品编号：Bellancom-15858A| CAS NO：2070014-95-6| 分子式：C₃₁H₄₄ClFN₈O₃| 分子量：631.18

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货号	价格	库存与货期
Bellancom-15858A	￥1100.00	杭州北京（现货）
Bellancom-15858A	￥2100.00	杭州北京（现货）
Bellancom-15858A	￥3400.00	杭州北京（现货）
Bellancom-15858A	￥7000.00	杭州北京（现货）
Bellancom-15858A	￥9900.00	杭州北京（现货）

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AP-III-a4 hydrochloride ENOblock hydrochloride

产品介绍

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 analogue enolase inhibitor with an IC₅₀ of 0.576 uM. AP-III-a4 hydrochloride can be used for the research of cancer and diabetic.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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

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

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

Cell Line:	HCT116
Concentration:	0.625, 1.25 and 2.5 μM
Incubation Time:	24 h
Result:	Inhibited cell migration dose-dependently.

RT-PCR

Cell Line:	Huh7 and HEK
Concentration:	10 μM
Incubation Time:	24 h
Result:	Induced glucose uptake and inhibited PEPCK expression.

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.

西域 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.

体内研究

AP-III-a4 (ENOblock) (10 μM; 96 h) inhibits cancer cell metastasis and suppresses the gluconeogenesis regulator PEPCK in zebrafish.

西域 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.

体内研究

AP-III-a4 (ENOblock) (10 μM; 96 h) inhibits cancer cell metastasis and suppresses the gluconeogenesis regulator PEPCK in zebrafish.

西域 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.

性状

Solid

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

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。