Methylenetetrahydrofolate dehydrogenase (MTHFD) is a key enzyme in the folate-dependent one carbon metabolism, which is important for the biosynthesis of several amino acids like glycine, alanine and serine, as well as nucleotide bases, formylated methionine and some pro-vitamins. In some bacteria like E. coli, MTHFD (called FolD in this species) is a dual function enzyme that catalyzes the conversion of 5,10-methylenetetrahydrofolate and NADP+ to 5,10-methenyltetrahydrofolate and NADPH (dehydrogenase function), and further converts the first product to 10-formyltetrahdrofolate (cyclohydrolase function). Some microorganisms have a separate enzyme for catalyzing the second cyclohydrolase function (FchA), and some species have an alternative pathway for 10-formyltetrahdrofolate production using formyltetrahydrofolate synthetase (Fhs). In eukaryotes, MTHFD is an important anticancer therapy target.
货号 | 产品名 | Cas | 产品描述 |
---|---|---|---|
PL07107 | DS18561882 | 2227149-22-4 | DS18561882 是一种高效的,对酶具有高选择性的亚甲基四氢叶酸脱氢酶 2 ( MTHFD2) 抑制剂,IC50 值为 0.0063 μM。DS18561882 抑制 MTHFD1 的 IC50 值是 0.57 μM。DS18561882 具有良好的口服药代动力学特性。 |
PL07105 | DS44960156 | 2361327-08-2 | DS44960156 是选择性的亚甲基四氢叶酸脱氢酶 2 (MTHFD2) 的抑制剂,其对 MTHFD2 和 MTHFD1 的 IC50 值分别为 1.6 μM 和 >30 μM。 |
PL07106 | LY 345899 | 10538-99-5 | LY 345899 是一种叶酸的类似物,也是一种亚甲基四氢叶酸脱氢酶 (MTHFD1; DC301) 和 MTHFD2 抑制剂,其 IC50 值分别为 96 nM 和 663 nM,对 MTHFD1 的 Ki 值为 18 nM。 |