纯度:98% by TLC,;NMR (Conforms)
分子式:C14H12N2O4S2
分子量:336.39
溶剂:DMSO (50 mg/ml) DMF (50 mg/ml)
性状:Off-white solid
存储:-20°C
Activity (short version):PHGDH / serine biosynthesis inhibitor
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.