Biochem/physiol Actions
NCT-503 is an inhibitor of phosphoglycerate dehydrogenase (PHGDH), which catalyzes the first, rate-limiting step of glucose-derived serine synthesis. NCT-503 reduced glucose-derived serine production and suppressed the growth of both PHGDH-dependent cancer cells in culture and in xenograft tumors, and caused G1/S cell cycle arrest in MDA-MB-468 cells. NCT-503 reduced the incorporation of one-carbon units from glucose-derived and exogenous serine into nucleotides, which may contribute to its anticancer activity. NCT-503 had an IC50 value of 2.5 µM for PHGDH and was inactive against a panel of other dehydrogenases and minimal cross-reactivity in a panel of 168 G-protein-coupled receptors (GPCRs). NCT-503 was found to be noncompetitive with respect to both 3-PG and NAD+, and exhibit good stability (>98% after 48 hrs in assay buffer) and aqueous solubility.
Packaging
5, 25 mg in glass bottle
Recommended products
NCT-503 Inactive Control, a structurally similar analog of NCT-503, is available from Sigma. To learn more about and purchase NCT-503 inactive control, click here.
| Colour | white to beige |
|---|---|
| Quality Level | 100 |
| InChI key | PJNSZIQUFLWRLH-UHFFFAOYSA-N |
| InChI | 1S/C20H23F3N4S/c1-14-11-15(2)24-18(12-14)25-19(28)27-9-7-26(8-10-27)13-16-3-5-17(6-4-16)20(21,22)23/h3-6,11-12H,7-10,13H2,1-2H3,(H,24,25,28) |
| Manufacturer | SIGMA-ALDRICH |
| Solubility | DMSO: 10 mg/mL, clear |
| Form | powder |
| Assay | ≥98% (HPLC) |
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