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Tocris Bioscience™ VER 246608
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Catalog No. 660410
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66-041-0 10 mg
66-045-0 50 mg
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Description

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.

Specifications

Chemical Name or Material 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
Quantity 10 mg
Target Other Kinase Inhibitors
Molecular Formula C28H23ClF2N4O4
Purity 0.98
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