chemical

VER 246608

6604/10

10 mg (also 50 mg)

213 USD

6604

6604/10

VER 246608

Potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3/4 inhibitor

Other Kinase Inhibitors

10 mg (also 50 mg)

Small Molecules

98%

Store at -20°C

552.96

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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.

VER246608 pan-isoform ATP competitive inhibitor inhibits pyruvate dehydrogenase kinase PDK PDHK cancer metabolism tumor microenvironment Other Kinases 6604,

Potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3/4 inhibitor

N-[4-(2-Chloro-5-methyl-4-pyrimidinyl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl]methyl]-2,4-dihydroxybenzamide

C28H23ClF2N4O4

C28H23ClF2N4O4

1684386-71-7

236

213 USD

Potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3/4 inhibitor