BI-4924 |
| カタログ番号GC35515 |
BI-4924 は、優れたミクロソーム安定性と肝細胞安定性を備えた、親油性の高血漿タンパク質結合選択的ホスホグリセリン酸デヒドロゲナーゼ (PHGDH) 阻害剤 (IC50=3 nM) です。 BI-4924 の細胞内トラッピングは、72 時間で 2200 nM の IC50 でセリン生合成を妨害します。
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Cas No.: 2244452-09-1
Sample solution is provided at 25 µL, 10mM.
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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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