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CBR-5884 | PHGDH / serine biosynthesis inhibitor

CAS:
681159-27-3
Catalog Number:
10-1588
Activity:
PHGDH inhibitor/ Blocks serine biosynthesis
Chemical Name:
Ethyl-5-(furan-carboxamido)-3-methyl-4-thiocyanatothiophene-2-carboxylate
Molecular Weight:
336.39
Molecular Formula:
C14H12N2O4S2
Solubility:
Soluble in DMSO (up to 50 mg/ml) or in DMF (up to 50 mg/ml).
Physical Properties:
Off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20°C for up to 2 months.
Shipping Code:
RT

CBR-5884 (681159-27-3) is a potent and selective inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), IC50=33 μM.1 The action of PHGDH is the first committed step of serine biosynthesis2 and certain cancer cells overexpress PHGDH3. CBR-5884 inhibits serine biosynthesis in cells with no effect on two other dehydrogenases, lactate dehydrogenase and MDH1 and without general cytotoxic effects up to 40 μM. CBR-5884 is selectively toxic to tumor cells with high serine synthesis activity. A novel tool for selective inhibition of serine biosynthesis in cells which also provides further proof that PHGDH is a viable target for the development of novel anticancer agents.1

References/Citations:

1) Mullarky et al. (2016), Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers; Proc. Natl. Acad. Sci. USA, 113 1778
2) Snell et al. (1986), The duality of pathways for serine biosynthesis is a fallacy; Trends Biochem. Sci., 11(6) 241
3) DeNicola et al. (2015), NFR2 regulates serine biosynthesis in non-small cell lung cancer; Nat. Genet., 47 1475

CBR-5884 | PHGDH / serine biosynthesis inhibitor is also available in the Cellular Metabolism Library.
CAS:
681159-27-3
Catalog Number:
10-1588
Activity:
PHGDH inhibitor/ Blocks serine biosynthesis
Chemical Name:
Ethyl-5-(furan-carboxamido)-3-methyl-4-thiocyanatothiophene-2-carboxylate
Molecular Weight:
336.39
Molecular Formula:
C14H12N2O4S2
Solubility:
Soluble in DMSO (up to 50 mg/ml) or in DMF (up to 50 mg/ml).
Physical Properties:
Off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20°C for up to 2 months.
Shipping Code:
RT

Safety Data Sheet:

Product Data Sheet:

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