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IC50: 2.5 μM for inhibiting serine synthesis from 3-phosphoglycerate in cells

NCT-503 is a 3-phosphoglycerate dehydrogenase (PHGDH) inhibitor.

In the canonical pathway of glucose-derived serine synthesis, Homo sapiens phosphoglycerate dehydrogenase (PHGDH) has been reported to catalyze the first, rate-limiting step.

In vitro: NCT-503 was identified as an inhibitor of PHGDH and was found to be inactive against a panel of other dehydrogenases and showed minimal cross-reactivity in a panel of G-protein-coupled receptors. In addition, treatment of three PHGDH-independent cell lines and five PHGDHdependent cell lines with NCT-503 demonstrated that NCT-503 had EC50 values of 8–16 μM for the PHGDH-dependent cell lines, and no toxicity toward other PHGDH-independent cell lines

IC50: 3.7 μM

NCT-502 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH).

Serine, a proteinogenic amino acid, is the source of one-carbon units essential for de novo purine and deoxythymidine synthesis. Homo sapiens phosphoglycerate dehydrogenase (PHGDH) catalyzes the first, rate-limiting step in the canonical pathway of glucose-derived serine synthesis.

In vitro: NCT-502 was identified as an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), inhibiting serine synthesis from 3-phosphoglycerate in cells. NCT-502 was inactive against a panel of other dehydrogenases and showed minimal cross-reactivity in a panel of 168 G-protein-coupled receptors. Moreover, In MDA-MB-231-PHGDH cells, NCT-502 treatment could decrease the intracellular serine and glycine concentrations and did not change the concentration of any other amino acid except for aspartate. In addition, NCT-502-mediated inhibition of serine synthesis was found to be reversible in cells [1].

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