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CBR-5884 | PHGDH / serine biosynthesis inhibitor

CBR-5884 (681159-27-3) is a potent and selective inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), IC50=33 μM1. 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 agents1

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) Snelll 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

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CBR-5884 is potent and selective inhibitor of 3-phosphoglycerate dehydrogenase

Catalog#  10-1588-0005

$70.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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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 as supplied. Solutions in DMSO or DMF may be stored at -20°C for up to 2 months.
Shipping Code:
RT
FeaturedDescription:
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.
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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