NCT-502 |
Catalog No.GC16860 |
NCT-502는 인간 PHGDH(포스포글리세르산 탈수소효소) 억제제로 PHGDH 의존성 암세포에 세포독성이 있으며 PHGDH에 대한 IC50이 3.7μM로 포도당 유래 세린 생성을 감소시킨다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1542213-00-2
Sample solution is provided at 25 µL, 10mM.
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].
In vivo: To evaluate the in-vivo activity NCT-503, a structurally close analog of NCT-502, NOD.SCID mice bearing MDA-MB-231 and MDA-MB-468 orthotopic xenografts were treated with vehicle or NCT-503. Results showed that NCT-503 reduced the growth and weight of PHGDH-dependent MDA-MB-468 xenografts but did not affect those of PHGDH-independent MDA-MB-231 xenografts. PHGDH inhibition caused by NCT-503 also selectively increased necrosis in MDA-MB-468 but not MDA-MB-231 xenografts. Importantly, mice treated with NCT-503 did not lose weight during the 24-d treatment [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Pacold, M. E.,Brimacombe, K.R.,Chan, S.H., et al. A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nature Chemical Biology 12(6), 452-458 (2016).
Average Rating: 5
(Based on Reviews and 32 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *