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PHGDH / serine biosynthesis inhibitor CAS#: 681159-27-3 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) title; Trends Biochem. Sci., 11 241 3) DeNicola et al. (2015) title; Nat. Genet., 47 1475

Product Code: ax44485 (5 mg)

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Product Specification

Function / pharmacology 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.
Chemical name Ethyl 5-(furan-2-carboxamido)-3-methyl-4-thiocyanatothiophene-2-carboxylate
Molecular weight 336.39
Molecular formula C14H12N2O4S2
Physical description Off-white solid
Solubility DMSO (50 mg/ml) DMF (50 mg/ml)
Size 5 mg
Stability Stable for 2 years as supplied. Solutions in DMSO or DMSO may be stored at -20 for up to 2 months.