Chemical Name: Ethyl 5-(furan-2-carboxamido)-3-methyl-4-thiocyanatothiophene-2-carboxylate
PHGDH / serine biosynthesis inhibitor
Molecular Weight:
336.39
Purity:
98% by TLC, NMR (Conforms)
Form:
Off-white solid
CAS Number:
[681159-27-3]
Formula:
C14H12N2O4S2
Application Notes:
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.
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