BI-4924 是一种亲脂性，与血浆蛋白高度结合的选择性磷酸甘油酸脱氢酶 (PHGDH) 抑制剂 (IC50=3 nM)，具有优异的微粒体和肝细胞稳定性。胞内捕获 BI-4924 可破坏丝氨酸生物合成，作用 72 小时的 IC50 为 2200 nM。
CAS：2244452-09-1
分子式：C21H20Cl2N2O6S
分子量：499.36
纯度：98%
存储：Store at -20°C

Background:

BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC50 of 2200 nM at 72 h[1]. PHGDH[1]

BI-4924 is a highly potent co-factor nicotinamide adenine dinucleotide (NADH/NAD+)-competitive PHGDH inhibitor. BI-4924 shows high selectivity against the majority of other dehydrogenase targets[1].

[1]. Weinstabl H, et al. Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor BI-4924 Disrupts Serine Biosynthesis. J Med Chem. 2019 Jul 31.