SML1659

NCT-503

≥98% (HPLC), phosphoglycerate dehydrogenase (PHGDH) inhibitor, powder

• Synonym(e): N-(4,6-Dimethylpyridin-2-yl)-4-(4-(trifluoromethyl)benzyl)piperazine-1-carbothioamide
• Empirische Formel (Hill-System): C₂₀H₂₃F₃N₄S
• CAS-Nummer: 1916571-90-8
• Molekulargewicht: 408.48
• UNSPSC Code: 12352200
• PubChem Substance ID: 329825998
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• Produktname: NCT-503, ≥98% (HPLC)
• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 10 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: CC1=CC(NC(N2CCN(CC3=CC=C(C(F)(F)F)C=C3)CC2)=S)=NC(C)=C1
• 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)
• InChI key: PJNSZIQUFLWRLH-UHFFFAOYSA-N

Beschreibung

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.

NCT-503 is an inhibitor of phosphoglycerate dehydrogenase (PHGDH).

Other Notes

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.

Sicherheitshinweise

• pictograms: GHS07
• signalword: Warning
• hcodes: H315
• pcodes: P264 - P280 - P302 + P352 - P332 + P313 - P362 + P364
• Hazard Classifications: Skin Irrit. 2
• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable