VER 246608

Product Description

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.

Solubility

Preparing Stock Solutions for VER 246608

The following data is based on the product molecular weight 552.96

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.81 mL	9.04 mL	18.08 mL
5 mM	0.36 mL	1.81 mL	3.62 mL
10 mM	0.18 mL	0.90 mL	1.81 mL
50 mM	0.04 mL	0.18 mL	0.36 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Moore VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. Oncotarget 2014 PMID: 25404640
• Brough Application of off-rate screening in the identification of novel pan- isoform inhibitors of pyruvate dehydrogenase kinase. J.Med.Chem. 2017 PMID: 28199108