VER-246608 is a potent (IC50s: PDK-1 = 35 nM, PDK-2 = 84 nM, PDK-3 = 40 nM, PDK-4 = 91 nM) and selective pan-pyruvate dehydrogenase kinase inhibitor.1 It decreased oxygen consumption and attenuated glycolytic activity (Warburg metabolism) under D-glucose/L-glutamine-depleted conditions. VER-246608 treatment of four cancer lines (PC-3, SW-1088, UM-22B, and MEF) under depleted D-glucose/L-glutamine conditions resulted in almost complete inhibition of cell growth. It also acted synergistically with doxorubicin in PC-3 and ES-2 cells.
* VAT and and shipping costs not included. Errors and price changes excepted