Powder: -20°C for 3 years | In solvent: -80°C for 1 year
VER-246608 is an effective and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (IC50s: 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively).VER-246608 disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. Consistent with a PDK mediated MOA, VER-246608 increased pyruvate dehydrogenase complex (PDC) activity, oxygen consumption and attenuated glycolytic activity. VER-246608 was found to potentiate the activity of doxorubicin.
説明 | VER-246608 is an effective and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (IC50s: 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively).VER-246608 disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. Consistent with a PDK mediated MOA, VER-246608 increased pyruvate dehydrogenase complex (PDC) activity, oxygen consumption and attenuated glycolytic activity. VER-246608 was found to potentiate the activity of doxorubicin. |
ターゲット&IC50 | PDK3:40 nM, PDK1:35 nM, PDK2:84 nM, PDK4:91 nM |
In vitro | 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 |
分子量 | 552.96 |
分子式 | C28H23ClF2N4O4 |
CAS No. | 1684386-71-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (90.42 mM)
You can also refer to dose conversion for different animals. 詳細
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VER-246608 1684386-71-7 Metabolism PI3K/Akt/mTOR signaling PDK Dehydrogenase Inhibitor PDHK VER246608 Pyruvate dehydrogenase kinase inhibit PDH kinase VER 246608 inhibitor