CBR-5884

CBR-5884 is a potent and selective inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH) (IC₅₀ = 33 μM) inhibiting serine synthesis from 3-phosphoglycerate in cells. CBR-5884 inhibits serine biosynthesis in cells with no effect on two other dehydrogenases, lactate dehydrogenase and MDH1 and without general cytotoxic effects up to 40 μM. CBR-5884 is selectively toxic to tumor cells with high serine synthesis activity.