2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Phosphoglycerate Dehydrogenase (PHGDH)

Phosphoglycerate Dehydrogenase (PHGDH)

Phosphoglycerate dehydrogenase (PHGDH) is involved in the early steps of L-serine synthesis in animal cells. L-Serine is a pivotal amino acid since it serves as a precursor to a large number of essential metabolites besides D-serine, a major agonist of the N-methyl-D-aspartate (NMDA) receptor. PHGDH is the first and only rate-limiting enzyme in the de novo serine biosynthetic pathway and catalyzes the oxidation of 3-PG derived from glycolysis to 3-phosphohydroxypyruvate (3-PHP). Mutations in PHGDH gene have been found in a family with congenital microcephaly, psychomotor retardation and other symptoms. An increase in PGDH levels, due to overexpression, is also associated with a wide array of cancers. In culture, PGDH is required for tumor cell proliferation, but extracellular L-serine is not able to support cell proliferation. This has led to the hypothesis that the pathway is performing some function related to tumor growth other than supplying L-serine.

Phosphoglycerate Dehydrogenase (PHGDH) Related Products (11):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-101966
    NCT-503
    		99.85%
    NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 2.5 µM.
    NCT-503
  • HY-100012
    CBR-5884
    		99.02%
    CBR-5884 is an active, selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) 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.
    CBR-5884
  • HY-117240
    NCT-502
    		99.18%
    NCT-502 is a human phosphoglycerate dehydrogenase (PHGDH) inhibitor, cytotoxic to PHGDH-dependent cancer cells, and reduces glucose-derived serine production, with an IC50 of 3.7 μM against PHGDH.
    NCT-502
  • HY-126253
    BI-4916
    		98.55%
    BI-4916 is a proagent of BI-4924. BI-4924 is a NADH/NAD+-competitive PHGDH inhibitor.
    BI-4916
  • HY-126254
    BI-4924
    		99.55%
    BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC50 of 2200 nM at 72 h.
    BI-4924
  • HY-121733
    PHGDH-inactive
    		99.72%
    PHGDH-inactive has no activity against PHGDH and serves as a negative control of NCT-502 and NCT-503.
    PHGDH-inactive
  • HY-123269
    PKUMDL-WQ-2101
    		Inhibitor 99.85%
    PKUMDL-WQ-2101 is a non-NAD+-competing allosteric phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 34.8 μM. PKUMDL-WQ-2101 exhibits antitumor activity.
    PKUMDL-WQ-2101
  • HY-148570
    PHGDH-IN-3
    		Inhibitor 98.99%
    PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer.
    PHGDH-IN-3
  • HY-123418
    PKUMDL-WQ-2201
    		Inhibitor 98.72%
    PKUMDL-WQ-2201 is a PHGDH non-NAD+-competing allosteric inhibitor (IC50=35.7 μM). PKUMDL-WQ-2201 also inhibits PHGDH mutants with IC50s of 69 μM (T59A) and >300 μM (T56AK57A), respectively. PKUMDL-WQ-2201 inhibits de novo serine synthesis in cancer cells, and reduces tumor growth.
    PKUMDL-WQ-2201
  • HY-145860
    PHGDH-IN-2
    PHGDH-IN-2 is a potent and NAD+ competitive PHGDH inhibitor with an IC50 of 5.2 µM. PHGDH-IN-2 inhibits the serine synthetic pathway in MDA-MB-468 cells. PHGDH-IN-2 inhibits the growth of PHGDH-dependent cancer cells.
    PHGDH-IN-2
  • HY-160252
    PHGDH-IN-4
    		Inhibitor
    PHGDH-IN-4 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-4 can be used for the research of cancer.
    PHGDH-IN-4