Koningic acid (KA) is a potent and selective inhibitor of glyceraldehyde-3-phosphate dehydrogenase (GAPDH).1 Inhibition is irreversible and proceeds via nucleophilic attack of an active site cysteine on the epoxide moiety2, Ki = 1.1 µM for rabbit muscle GAPDH3. KA can selectively kill high-glycolytic cancer cells via glucose dependent ATP depletion.4 Has been used in a predictive model for selective targeting of the Warburg effect, the most prominent hallmark of cancer cell metabolism.5
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