BI-4924 |
Catalog No.GC35515 |
Le BI-4924 est un inhibiteur sélectif de la phosphoglycérate déshydrogénase (PHGDH) lipophile, fortement lié aux protéines plasmatiques (IC50 = 3 nM) avec une excellente stabilité microsomale et hépatocytaire. Le piégeage intracellulaire du BI-4924 perturbe la biosynthèse de la sérine avec une IC50 de 2200 nM À 72 h.
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Cas No.: 2244452-09-1
Sample solution is provided at 25 µL, 10mM.
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.
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