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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]. | [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]. | 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. |
| [References]
[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. DOI:10.1016/j.bcp.2018.07.004
[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. DOI:10.1038/s41598-019-40885-z
[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). DOI:10.1038/srep23793
[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. DOI:10.3390/cancers10100391 |
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