化合物VER-246608 T17224

Product Introduction
Bioactivity


英文名: VER-246608

描述: VER-246608 是ATP 竞争性的丙酮酸脱氢酶激酶抑制剂，对PDK-1，PDK-3，PDK-2，和PDK-4的IC50分别为 35 nM，40 nM，84 nM 和 91 nM。

体外活性: A novel and selective ATP competitive pan-isoform inhibitor of PDK, VER-246608.?Consistent with a PDK mediated MOA, VER-246608 increased pyruvate dehydrogenase complex (PDC) activity, oxygen consumption and attenuated glycolytic activity.?However, these effects were only observed under D-glucose-depleted conditions and required almost complete ablation of PDC E1α subunit phosphorylation.?VER-246608 was weakly anti-proliferative to cancer cells in standard culture media

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (90.42 mM)


关键字: Inhibitor | PDHK | VER-246608 | VER246608 | Pyruvate dehydrogenase kinase | inhibit | PDH kinase | VER 246608

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相关库: Anti-Prostate Cancer Compound Library | Glycometabolism Compound Library | Oxidation-Reduction Compound Library | Anti-Cancer Compound Library | Neuronal Differentiation Compound Library | Antidepressant Compound Library | Kinase Inhibitor Library | Inhibitor Library | Metabolism Compound Library | Anti-Pancreatic Cancer Compound Library

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