VB124 is a selective, highly potent MCT4 inhibitor, blocks lactate import (IC50 =8.6 nM) and export (IC50=19 nM) in MDA-MB-231 cells.
VB124 is highly selective for MCT4 over MCT1, showing very little MCT1 inhibitory activity (IC50=24 μM) in MCT1-expressing BT20 cells.
VB124 prevents and reverses hypertrophy in cardiomyocytes, prevents the increased flux from glucose into pyruvate and intra- and extracellular lactate observed in PE- and ISO-treated cardiomyocytes.
VB124 replenishes mitochondrial pyruvate flux, improves mitochondrial membrane potential and mitigates cytosolic ROS.
VB124 prevents cardiac hypertrophy in mice.
