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VER 246608

Catalog #: 6604 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
6604/10
6604/50
VER 246608 | CAS No. 1684386-71-7 | Other Kinase Inhibitors
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Description: Potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3/4 inhibitor

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

Purity: ≥98%

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Biological Activity

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.

Technical Data

M.Wt:
552.96
Formula:
C28H23ClF2N4O4
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
1684386-71-7

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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