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

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.

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.

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.

PHGDH-IN-6 (Compound L5) acts as an allosteric inhibitor of PHGDH, with an IC50 of 2.5 μM. It is applicable in the study of diseases related to serine synthesis.

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].

Z1609609733 (Compound 18) is a non-covalent inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH) with an IC50 of 1.46 μM. It effectively suppresses serine synthesis, interferes with cancer metabolism, and completely halts cell proliferation.

DGY-09-192 is a PROTAC FGFR1/2 degrader with DC50 values of 4.35 nM for FGFR1 and 70 nM for FGFR2. It selectively degrades wild-type FGFR1/2 and various FGFR2 fusion proteins, including FGFR2-PHGDH and FGFR2-OPTN. In both in vitro and in vivo studies, DGY-09-192 inhibits downstream FGFR signaling pathways by reducing the phosphorylation of FRS2Y196 and ERK1/2T202/Y204.

PKUMDL-WQ-2201 is a PHGDH non-NAD⁺-competing allosteric inhibitor with micromolar potency against wild-type and mutant PHGDH enzymes, effectively suppressing de novo serine biosynthesis in cancer cells and reducing tumor growth, PKUMDL-WQ-2201 provide a metabolic intervention strategy for studying serine-dependent tumor metabolism.

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