CBR-5884 (681159-27-san) 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
CBR-5884(681109 -27-san)是一种高效的选择性3-磷酸甘油酸脱氢酶抑制剂，IC50=33 μM.1 phgdhh的作用是丝氨酸生物合成的第一步2，某些癌细胞过表达PHGDH3。 CBR-5884抑制细胞丝氨酸生物合成，但不影响其他两种脱氢酶，乳酸脱氢酶和MDH1，且不产生一般的细胞毒性作用，最高可达40 μM。 CBR-5884对具有较高丝氨酸合成活性的肿瘤细胞具有选择性毒性。 一种选择性抑制细胞丝氨酸生物合成的新工具，这也进一步证明了PHGDH是开发新型抗癌药物的一个可行靶点 。

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

CAS:
681159-27-三
Catalog Number:
10-1588
Activity:
PHGDH inhibitor/Blocks serine biosynthesis
Chemical Names:
Ethyl-5-(furancarboxamido)-3-methyl-4-thiocyanatothiophene-2-carboxylate
Molecular Weight:
336.39
Molecular Formula:
C₁₄H₁₂N₂O₄S₂
Solubility:
Soluble in DMSO (50 mg/ml); DMF (50 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% 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 3 months.
Shipping Code:
RT