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Description

A cell-permeable alpha-cyanocinnamate compound that acts as a rapid, active site thiol modifying, time-dependent and non-competitive inhibitor of bi-directional pyruvate transport across plasma membranes in yeast, bacteria, Drosophila, and humans (IC50 = 50 nM in rat heart mitochondria, Ki <= 1 µ,M) with excellent selectivity over monocarboxylates and anions. Shown to significantly decrease pyruvate-driven respiration, enhance glucose uptake and activate AMPK (2 µ,M in human myocytes and skeletal muscle myotubes).