CB-839 (CAS: 1439399-58-2) 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. By blocking glutamine utilization, proliferation in rapidly growing cells is impaired. Glutamine-dependent tumors rely on the conversion of exogenous glutamine into glutamate and glutamate metabolites to both provide energy and generate building blocks for the production of macromolecules, which are needed for cellular growth and survival.
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TGF-beta/Smad
Phospholipase
