Potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3/4 inhibitor
VER 246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK; IC50s = 35, 40, 84, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4 respectively). It is selective for PDKs over a panel of 97 kinases and HSP90. VER 246608 increases pyruvate dehydrogenase complex activity, oxygen consumption and reduces glycolytic activity; it reduces the production of L-lactate in PC3 cells in D-glucose and L-glutamine depleted media. In PC3 cells, VER 246608 induces cell cycle arrest at the G1 phase under glucose or serum-depleted conditions characteristic of the tumor microenvironment.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-124555 |
| Réf. fabricant | 18759926 |
| Nom chimique ou matériau | N-[4-(2-Chloro-5-methyl-4-pyrimidinyl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl]methyl]-2,4-dihydroxybenzamide |
| CAS | 1684386-71-7 |
| Quantité | 50 mg |
| Cible | Other Kinase Inhibitors |
| Formule moléculaire | C<sub>28</sub>H<sub>23</sub>ClF<sub>2</sub>N<sub>4</sub>O<sub>4</sub> |
| Pureté | 0.98 |
