Description
EB-3D is a novel potent and selective choline kinase ChoKalpha inhibitor with IC50 of 1.0uM (purified ChoKalpha1), strongly impairs cell proliferation in a variety of different cancer cell lines; demonstrates in vitro antiproliferative effects against HeLa (IC50=79nM), RS4, 11 (IC50=45nM), A549 (IC50=27nM) and MDA-MB-231 (IC50=100nM); displays excellent antiproliferative activity against a wide cohort of T-leukemic cell lines with GI50 of 0.9nM (MOLT-16 cell)-479nM (CCRF-CEM), reduces the intracellular pool of PCho, but also inhibits the synthesis of choline-containing lipids; induces G0/G1 arrest that lead to apoptosis in leukemia cell lines; affects AMPK-mTOR signaling pathway, synergizes with both dexamethasone and L-asparaginase