上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
| 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].
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IC50 & Target |
IC50: 1 μM; Kd: 0.7 μM[3]
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体外研究
(In Vitro) |
EB-3D displays (0-100 μM; 72 hours) excellent antiproliferative activity against a wide cohort of T-leukemic cell lines, with GI GI50s 13 values in the nanomolar range[1].
EB-3D (1.25-5μM; 24 hours) induced apoptosis in leukemia cell lines[1].
EB-3D (0.5-1 μM; 24 hours) induces a G0/G1 arrest that lead to apoptosis[1].
EB-3D (0.3 μM; 48 hours) shows a first spike of activation of AMPKα after 30 minutes and a later increase in the phosphorylation of T172[1].
EB-3D (1-40 μM; 48 hours) inhibits cell growth in HepG2 cells with a GI50 of 14.55 μM[2].
EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells[1].
上海金畔生物科技有限公司 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. |
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体内研究
(In Vivo) |
EB-3D (1 mg/kg; i.p.; every other day) impairs mammary tumor growth in syngeneic orthotopic E0771-C57BL/6 mouse model[4].
EB-3D (2.5 mg/kg; every other day for 4 weeks) shows a reduction of the number of spontaneous lung macro- and micrometastasis[4].
上海金畔生物科技有限公司 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. |
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| 分子量 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 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)
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| 溶解性数据 |
In Vitro:
DMSO : 50 mg/mL (77.59 mM; Need ultrasonic)
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 |
| 10 mM |
0.1552 mL |
0.7759 mL |
1.5517 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。
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| 参考文献 |
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[1]. Mariotto E, et al. EB-3D a novel choline kinase inhibitor induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells. Biochem Pharmacol. 2018 Sep;155:213-223.
[2]. Sola-Leyva A, et al. Choline kinase inhibitors EB-3D and EB-3P interferes with lipid homeostasis in HepG2 cells. Sci Rep. 2019 Mar 25;9(1):5109.
[3]. Schiaffino-Ortega S, et al. Design, synthesis, crystallization and biological evaluation of new symmetrical biscationic compounds as selective inhibitors of human Choline Kinase α1 (ChoKα1).
[4]. Mariotto E, et al. Choline Kinase Alpha Inhibition by EB-3D Triggers Cellular Senescence, Reduces Tumor Growth and Metastatic Dissemination in Breast Cancer. Cancers (Basel). 2018;10(10):391. Published 2018 Oct 22.
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