| Name | VER-246608 |
| Description | 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. |
| 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 |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.62 mM), Sonication is recommended. DMSO : 50 mg/mL (90.42 mM), Sonication is recommended.
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| Keywords | VER-246608 | VER246608 | VER 246608 | Pyruvate dehydrogenase kinase | PDK-4 | PDK4 | PDK-3 | PDK3 | PDK-2 | PDK2 | PDK-1 | PDK1 | PDHK | PDH kinase | PDH | Inhibitor | inhibit |
| Inhibitors Related | Disulfiram | Mycophenolate Mofetil | Rotenone | Ribavirin | 18β-Glycyrrhetinic acid | Benzyl alcohol | 2-Methylaminoethanol | Methotrexate disodium | Dimethyl malonate | Isomalt | D-Mannitol | Ethyl potassium malonate |
| Related Compound Libraries | Anti-Lung Cancer Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Autophagy Compound Library | Anti-Breast Cancer Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Fibrosis Compound Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library |