CB-839CB-839 is a potent, selective, and orally bioavailable inhibitor of both splice variants of glutaminase (KGA and GAC); inhibits recombinant GAC with an IC50 of <15 nM.
IC50 value: <15 nM(GAC) [1]
Target: glutaminase inhibitor
CB-839 had antiproliferative activity in a triple-negative breast cancer (TNBC) cell line, HCC-1806, that was associated with a marked decrease in glutamine consumption, glutamate production, oxygen consumption, and the steady-state levels of glutathione and several tricarboxylic acid cycle intermediates.
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