LY374571

LY374571 is an experimental small molecule inhibitor that targets enzymes involved in folate metabolism. It is a glutamic acid derivative designed to inhibit human methylenetetrahydrofolate dehydrogenase/cyclohydrolase (MTHFD1), a key enzyme in one-carbon metabolism and nucleotide biosynthesis[1][8][9]. The compound has been used as a tool molecule for biochemical studies and structure-based drug design targeting folate-dependent enzymes. While it demonstrates inhibitory activity against MTHFD1 and related enzymes such as FolD (bifunctional methylenetetrahydrofolate dehydrogenase/cyclohydrolase), it has not advanced beyond preclinical or early pharmacokinetic evaluation[8][9]. Its mechanism of action involves competitive inhibition at the active site of these oxidoreductases/hydrolases critical for purine and amino acid biosynthesis.

Other names

(2S)-2-((4-(((2,5-diamino-6-oxo-3,6-dihydropyrimidin-4-yl)carbamoyl)amino)phenyl)formamido)pentanedioic acid(2S)-2-[(4-{[(2,5-diamino-6-oxo-3,6-dihydropyrimidin-4-yl)carbamoyl]amino}phenyl)formamido)pentanedioic acid[[N'-(2,5-DIAMINO–6-HYDROXY-PYRIMIDIN–4-YL)-UREAYL]-PHEN–4-YL]-CARBONYL–GLUTAMIC ACIDN–[(4-{[(2,5-diamino–6-hydroxypyrimidin–4‑yl)carbamoyl]amino}phenyl)carbonyl]‑L‑glutamic acid