Catalog No.: PC-24275Not For Human Use, Lab Use Only.
VER-246608 is a potent, pan-isoform ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK, PDHK) with IC50 of 35 nM, 40 nM, 84 nM, and 91 nM for PDHK1, PDHK3, PDHK2, and PDHK4, respectively.
VER-246608 is a potent, pan-isoform ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK, PDHK) with IC50 of 35 nM, 40 nM, 84 nM, and 91 nM for PDHK1, PDHK3, PDHK2, and PDHK4, respectively. VER-246608 increases pyruvate dehydrogenase complex (PDC) activity, oxygen consumption and attenuated glycolytic activity. VER-246608 is weakly anti-proliferative to cancer cells in standard culture media; however, depletion of either serum or combined D-glucose/L-glutamine resulted in enhanced cellular potency. VER-246608 potentiates the activity of doxorubicin. VER-246608 disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells.
