CBR-5884 is an selective, active of phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis. Biochemical characterization of the inhibitor revealed that it was a noncompetitive inhibitor that showed a time-dependent onset of inhibition and disrupted the oligomerization state of PHGDH

PHGDH:33 μM

CBR-5884 (15 or 30 μM; 3-5 days) selectively inhibits breast cancer lines that have a high propensity for serine synthesis. CBR-5884 (15 or 30 μM; 3-5 days) also selectively inhibits the proliferation of melanoma.