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 诱导白血病 T 细胞中 AMPK-mTOR 通路解除和凋亡 (apoptosis)。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。
| Cas No. | 1839150-63-8 |
| Canonical SMILES | CN(C1=CC=[N+](CC2=CC=C(OCCOC3=CC=C(C[N+]4=CC=C(N(C)C)C=C4)C=C3)C=C2)C=C1)C.[Br-].[Br-] |
| 分子式 | C30H36Br2N4O2 |
| 分子量 | 644.44 |
| 溶解度 | DMSO: 50 mg/mL (77.59 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity[1][2][3]. [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). |
