CBR-5884 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), inhibiting serine synthesis from 3-phosphoglycerate in cells with an IC50 value of 33 μM. It does not affect other NAD+-dependent dehydrogenases, including lactate dehydrogenase and malate dehydrogenase 1. CBR-5884 inhibits the proliferation of cancer cells by blocking de novo serine synthesis and is selectively cytotoxic for cells with high serine biosynthetic activity.
