phgdh

PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 2.8 μM against PHGDH, and it can be used in cancer research.

inactive analog of the 3-phosphoglycerate dehydrogenase (PHGDH) inhibitors NCT-502 and NCT-503

PHGDH-IN-2 is a potent NAD+-competitive PHGDH inhibitor (IC50: 5.2 μM) that exhibits inhibitory effects on the growth of PHGDH-dependent cancer cells and inhibits the serine synthesis pathway in [MDA-MB-468] cells.

PHGDH-IN-4, a phosphoglycerate dehydrogenase (PHGDH) inhibitor, can be used for cancer research [1].

Compound B12 (PHGDH-IN-5) acts as a covalent inhibitor of PHGDH, demonstrating an IC50 value of 0.29 μM. It has been shown to inhibit the proliferation of cancer cell lines that overexpress PHGDH and reduce the production of glucose-derived serine in MDA-MB-468 cells [1].

NCT-502 (N-(4,6-dimethylpyridin-2-yl)-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine-1-carbothioamide) is a human phosphoglycerate dehydrogenase inhibitor, cytotoxic to PHGDH-dependent cancer cells. It decreases glucose-derived serine production and it has an IC50 of 3.7 μM against PHGDH.

NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=2.5 µM) with no activity against other dehydrogenases. NCT-503 has antitumor activity and inhibits the growth of PHGDH-dependent tumors.

BI-4916 is a selective phosphoglycerate dehydrogenase (PHGDH) inhibitor that inhibits SSP and reduces the migration of cancer cells.BI-4916 can be used in the study of cancer and metabolic diseases.

BI-4924 is a selective and potent inhibitor of phosphoglycerate dehydrogenase (PHGDH) (IC50=3 nM) that disrupts serine biosynthesis by intracellular trapping, and can be used in the study of diseases caused by dysfunction.

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

PKUMDL-WQ-2101 is a selective allosteric inhibitor of phosphoglycerate dehydrogenase with anti-tumor activity.

PKUMDL-WQ-2201 is a selective allosteric inhibitor of phosphoglycerate dehydrogenase (PHGDH) with Anti-tumor Activity, it binds to site II.

DNS-pE is the first small molecule that can selectively label endogenous 3-phosphoglycerate dehydrogenase (PHGDH) from various mammalian cells.