1. Autophagy
  2. Autophagy
  3. EN6

EN6 是一种小分子体内自噬 (autophagy) 激活剂,其共价靶向溶酶体v-ATP 酶的 ATP6V1A 亚基中的半胱氨酸 277。EN6 介导的 ATP6V1A 修饰使 v-ATP 酶与 Rag 解偶联,导致 mTORC1 信号的抑制,增加溶酶体酸化,并激活自噬。EN6 还能以溶酶体依赖的方式清除 TDP-43 聚集物 (额颞叶痴呆的致病因子)。

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EN6 Chemical Structure

EN6 Chemical Structure

CAS No. : 1808714-73-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1013
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1 mg ¥368
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5 mg ¥921
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10 mg ¥1567
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50 mg ¥3135
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100 mg ¥4700
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500 mg   询价  

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EN6 is a small-molecule in vivo autophagy activator that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase. EN6-mediated modification of ATP6V1A uncouples v-ATPase from Rag, leading to inhibition of mTORC1 signalling, increased lysosomal acidification, and activation of autophagy. EN6 also scavenges TDP-43 aggregates (causative agents of frontotemporal dementia) in a lysosome-dependent manner[1].

体外研究
(In Vitro)

在 HEK293A 细胞中,EN6 (50 μM; 1, 4, 8 h) 增加 LC3BII 的水平,并以时间和剂量依赖的方式触发 LC3 斑点的形成[1]
EN6 导致 HEK293A 细胞中自噬体和自噬溶酶体数量显著增加[1]
EN6 (25 μM;1 h) 阻断 HEK293A 细胞中的 mTORC1 溶酶体定位和激活[1]
EN6 (50 μM;4 h) 激活 HEK293A 细胞中的 v-ATPase 和溶酶体酸化[1]
EN6 (25 μM;7 h) 促进 IPTG 诱导的 GFP-TDP43 U2OS 骨肉瘤细胞系模型中蛋白质聚集体的自噬清除[1]

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

Western Blot Analysis[1]

Cell Line: HEK293A cells
Concentration: 50 μM
Incubation Time: 1, 4, 8 h
Result: Time- and dose-dependently triggered formation of LC3 puncta and increased the levels of LC3BII.

Western Blot Analysis[1]

Cell Line: HEK293A cells
Concentration: 25 μM
Incubation Time: 1 h
Result: Led to complete inactivation of mTORC1 signaling, as shown by reduced levels of phosphorylated canonical substrates, S6 kinase 1 (S6K1), 4EBP1, and ULK1.

Immunofluorescence[1]

Cell Line: HEK293A cells
Concentration: 50 μM
Incubation Time: 4 h
Result: Led to significantly increased acidification of the lysosome in HEK293A cells, and this heightened acidification was blocked by BafA1.

Immunofluorescence[1]

Cell Line: IPTG-inducible GFP-TDP43 U2OS osteosarcoma cell line model
Concentration: 25 μM
Incubation Time: 7 h
Result: Reduced IPTG-induced TDP43 aggregates by 75 %.
体内研究
(In Vivo)

EN6 (50 mg/kg; i.p.; single) 在体内抑制 mTORC1 并激活自噬[1]

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

Animal Model: Six-week-old male C57BL/6 mice[1].
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; single
Result: Significantly inhibited mTORC1 signaling in both skeletal muscle and heart, as demonstrated by reduced phosphorylation of S6, 4EBP1 and ULK1.
Strongly activated autophagy as shown by heightened LC3BII levels and reduced p62 levels.
分子量

368.34

Formula

C19H14F2N4O2

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 5 mg/mL (13.57 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

Ethanol 中的溶解度 : 1.11 mg/mL (3.01 mM; 超声助溶 (<60°C))

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7149 mL 13.5744 mL 27.1488 mL
5 mM 0.5430 mL 2.7149 mL 5.4298 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂: 50% PEG300    50% Saline

    Solubility: 10 mg/mL (27.15 mM); 悬浊液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

EN6 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.7149 mL 13.5744 mL 27.1488 mL 67.8721 mL
DMSO 5 mM 0.5430 mL 2.7149 mL 5.4298 mL 13.5744 mL
10 mM 0.2715 mL 1.3574 mL 2.7149 mL 6.7872 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
EN6
目录号:
HY-128892
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