EB-3D

EB-3D is a novel, potent, and selective small molecule inhibitor of choline kinase alpha (ChoKα), specifically targeting the ChoKα1 isoform with an IC50 of approximately 1 μM. Choline kinase catalyzes the first step of the Kennedy pathway, phosphorylating choline to phosphocholine, which is essential for phosphatidylcholine synthesis and cell membrane division. Developed collaboratively by researchers at the University of Padova, the University of Brescia, and the University of Granada, EB-3D has demonstrated significant preclinical efficacy in oncology. In breast cancer models, including triple-negative breast cancer (TNBC), EB-3D treatment reduces phosphocholine levels, induces G0/G1 cell cycle arrest, and triggers irreversible cellular senescence via activation of the AMPK pathway and subsequent downregulation of the mTORC1 pathway. Additionally, EB-3D has shown potent antiproliferative activity in T-cell acute lymphoblastic leukemia (T-ALL) and HepG2 liver cancer models, and has demonstrated in vivo efficacy by reducing tumor growth and spontaneous lung metastasis in syngeneic orthotopic mouse models.

Other names

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(dimethylamino)pyridinium) bromide1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(dimethylamino)pyridinium) dibromide