1. PI3K/Akt/mTOR Epigenetics Apoptosis
  2. AMPK Apoptosis
  3. EB-3D

EB-3D 是有效的选择性胆碱激酶 α (ChoKα) 抑制剂,对 ChoKα1 的 IC50 值为 1 μM。EB-3D 对 ChoKα 表达、AMPK 激活、细胞凋亡 (apoptosis)、内质网应激和脂质代谢有影响。EB-3D 在一组T-白血病细胞系中显示出强大的抗增殖活性。具有抗癌活性。

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EB-3D Chemical Structure

EB-3D Chemical Structure

CAS No. : 1839150-63-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2694
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1 mg ¥952
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5 mg ¥1900
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10 mg ¥3000
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25 mg ¥5000
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity[1][2][3].

IC50 & Target

IC50: 1 μM; Kd: 0.7 μM[3]

体外研究
(In Vitro)

EB-3D 显示 (0-100 μM;72 小时) 对广泛的 T 白血病细胞系具有出色的抗增殖活性,GI GI50s 13 值在纳摩尔范围内[1]
EB-3D (1.25-5 μM;24小时) 诱导白血病细胞系凋亡[1]
EB-3D (0.5-1 μM;24 小时) 诱导导致细胞凋亡的 G0/G1 期阻滞[1]
EB-3D (0.3 μM;48 小时) 在 30 分钟后显示 AMPKα 激活的第一个尖峰以及随后 T172[1] 的磷酸化增加。
EB-3D (1-40 μM;48 小时) 抑制 HepG2 细胞的细胞生长,GI50 14.55 μM[2]
EB-3D 诱导 AMPK-mTOR 通路失调和白血病 T 细胞凋亡[1]

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

Cell Proliferation Assay[1]

Cell Line: JURKAT, CCRF-CEM, HSB-2, MOLT-16, DNA-41, LOUCY, PEER, ALL-SIL cells
Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 72 hours
Result: Inhibited JURKAT, CCRF-CEM, HSB-2, MOLT-16, DNA-41, LOUCY, PEER, and ALL-SIL cells growth with GI50s of 136.2, 478.8, 17.7, 0.9, 60.6, 200, 265, and 132 nM, respectively.

Apoptosis Analysis[1]

Cell Line: Jurkat, CCRF-CEM and HSB-2 cells
Concentration: 1.25, 2.5, 5 μM
Incubation Time: 24 hours
Result: Induced apoptosis in leukemia cell lines.

Cell Cycle Analysis[1]

Cell Line: Jurkat, CCRF-CEM and HSB-2 cells
Concentration: 0.5, 1 μM
Incubation Time: 24 hours
Result: Induces cell cycle arrest in G0/G1 phase.

Western Blot Analysis[1]

Cell Line: Jurkat cells
Concentration: 0.3 μM
Incubation Time: 48 hours
Result: Showed a first spike of activation of AMPKα after 30 minutes of treatment and a later increase in the phosphorylation of T172. The increase in S79 phosphorylation of its main target ACC (acetyl-coenzyme A (CoA) carboxylase), followed the same pattern. This rapid activation of AMPK, in turn induced a consequent reduction in mTOR phosphorylation that is visible already at 30’ and that becomes amplified at longer time probably due to the interruption of feedback loops that are characteristic of mTOR connecting pathways.
体内研究
(In Vivo)

EB-3D (1 mg/kg;腹腔注射;每隔一天) 在同源原位 E0771-C57BL/6 小鼠模型中抑制乳腺肿瘤的生长[4]
EB-3D (2.5 mg /kg;每隔一天,持续 4 周) 显示自发性肺大转移和微转移的数量减少[4]

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

Animal Model: E0771-C57BL/6 mice[4]
Dosage: I.p.; every other day for 4 weeks
Administration: 2.5 mg/kg
Result: A reduction of the number of spontaneous lung macro- and micrometastasis.
分子量

644.44

Formula

C30H36Br2N4O2

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

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
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (77.59 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)

H2O 中的溶解度 : ≥ 9.09 mg/mL (14.11 mM)

* "≥" 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 1.5517 mL 7.7587 mL 15.5173 mL
5 mM 0.3103 mL 1.5517 mL 3.1035 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, 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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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

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

纯度: 99.57%

参考文献

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, 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.5517 mL 7.7587 mL 15.5173 mL 38.7934 mL
5 mM 0.3103 mL 1.5517 mL 3.1035 mL 7.7587 mL
10 mM 0.1552 mL 0.7759 mL 1.5517 mL 3.8793 mL
DMSO 15 mM 0.1034 mL 0.5172 mL 1.0345 mL 2.5862 mL
20 mM 0.0776 mL 0.3879 mL 0.7759 mL 1.9397 mL
25 mM 0.0621 mL 0.3103 mL 0.6207 mL 1.5517 mL
30 mM 0.0517 mL 0.2586 mL 0.5172 mL 1.2931 mL
40 mM 0.0388 mL 0.1940 mL 0.3879 mL 0.9698 mL
50 mM 0.0310 mL 0.1552 mL 0.3103 mL 0.7759 mL
60 mM 0.0259 mL 0.1293 mL 0.2586 mL 0.6466 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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:
EB-3D
目录号:
HY-115463
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