|1,1'-(((乙烷-1,2-二基双(氧基))双(4,1-亚苯基))双(亚甲基))双(4-(二甲氨基)吡啶-1-鎓)溴化物|CsnPharm

CAS No.: 1839150-63-8

EB-3D Catalog No. CSN25346

EB-3D is a novel potent and selective choline kinase ChoKα inhibitor with an IC50 of 1 μM. EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells and induces senescence in breast cancer cell lines through the activation of the metabolic sensor AMPK and the subsequent dephosphorylation of mTORC1 downstream targets.

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技术信息

生物活性

描述Choline kinase (ChoK) catalyzes the phosphorylation of choline by ATP in the presence of Mg²⁺ to yield phosphocholine (PCho) and ADP. In humans, ChoKα1 and ChoKα2 derive from a single gene (chk-α) by alternative splicing. EB-3D, a potent and selective ChoKα inhibitor, shows an IC₅₀ of 1 μM for human ChoKα1. In a panel of nine different human tumor-cell lines, EB-3D offered excellent antiproliferative activities against all cell lines with GI₅₀ values ranging from 0.027 to 0.12 μM. The cell viability in the presence of EB-3D was also evaluated in Jurkat, HeLa and MDA-MB-231 cell lines. EB-3D significantly inhibited cell growth in three cell lines in a concentration-dependent manner. EB-3D induced a G1 arrest of the cell cycle, which occurred in a concentration-dependent manner in the three cell lines tested (Jurkat, MCF-7 and MDA-MB-231). Together with the G1 increase, a concomitant reduction was found in the S phase. Further, EB-3D at different concentrations after 72 h of incubation induced a modest increment in apoptotic cells only in Jurkat cells^[1]. Experimental metastasis models obtained after the iv injection of murine E0771 or human MDA-MB-231 cells were treated with EB-3D at the dose of 2.5 mg/kg. After lung removal, the number of macrometastases as well as of micrometastases was significantly reduced in treated mice when compared with control lungs. In addition, a significant reduction of resected lung weight was appreciable after EB-3D treatment^[2].
作用机制The 1-benzyl-4-(dimethylamino)pyridinium fragment of EB-3D performs a strong π-cation interaction with the Cho binding site^[1].
参考文献

[1] Schiaffino-Ortega S, Baglioni E, Mariotto E, et al. Design, synthesis, crystallization and biological evaluation of new symmetrical biscationic compounds as selective inhibitors of human Choline Kinase α1 (ChoKα1). Sci Rep. 2016;6:23793
[2] Mariotto E, Viola G, Ronca R, 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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 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

技术信息

CAS号

1839150-63-8

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H36Br2N4O2

运输

蓝冰

分子量

644.44

别名

溶解度

DMSO	48.0 mg/mL (74.5 mM)
Water	24.0 mg/mL (37.2 mM)
Ethanol	15.0 mg/mL (23.3 mM)

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