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NCT-503
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C20H23F3N4S
- MW: 408.48
Description
NCT-503 is a potent and non-competitive phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 value of 2.5 μM. NCT-503 reduces the production of glucose-derived serine in cells and suppresses the growth of PHGDH-dependent cancer cells in culture and orthotopic xenograft tumor models.
PHGDH catalyzes the first committed step in the de novo serine biosynthesis pathway and is frequently upregulated in metabolically dependent cancers. NCT-503 is an optimized in vivo chemical probe with improved potency and solubility compared to the earlier PHGDH inhibitor NCT-502, making it a valuable tool for studying cancer metabolism and serine biosynthesis.
Key Features
- Potent non-competitive PHGDH inhibitor
- IC50: 2.5 μM
- Reduces glucose-derived serine production
- Suppresses growth of PHGDH-dependent cancer cells
- Optimized in vivo probe with improved solubility
Applications
- PHGDH and serine biosynthesis research
- Cancer metabolism studies
- Metabolic pathway analysis
- Tumor growth and xenograft models
- Non-small cell lung cancer (NSCLC) research
Sold under license from Whitehead Institute for Biomedical Research, DFCI and NIH.
More Information
| Parent CAS No. | 1916571-90-8 |
|---|---|
| Chemical Name | N-(4,6-dimethylpyridin-2-yl)-4-(4-(trifluoromethyl)benzyl)piperazine-1-carbothioamide |
| SMILES | N1(C(=S)NC2=NC(C)=CC(C)=C2)CCN(CC2=CC=C(C(F)(F)F)C=C2)CC1 |
| MFCD | N.A. |
| InChi | 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) |
| InChiKey | PJNSZIQUFLWRLH-UHFFFAOYSA-N |
| CID | 118796328 |
| Short Description | PHGDH inhibitor |
References
- ME Pacold et al. A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nat Chem Biol. 2016 Jun;12(6):452-8.
- JE Unterlass et al. Validating and enabling phosphoglycerate dehydrogenase (PHGDH) as a target for fragment-based drug discovery in PHGDH-amplified breast cancer. Oncotarget. 2016 Aug 22.
- JM Rohde et al. Discovery and optimization of piperazine-1-thiourea-based human phosphoglycerate dehydrogenase inhibitors. Bioorg Med Chem. 2018 May 1;26(8):1727-1739.
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