EB-3D

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] 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]. 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].