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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.
VER 246608 is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 will affect the solvent volumes required to prepare stock solutions.
|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||0.9 mL||1.81 mL|
|50 mM||0.04 mL||0.18 mL||0.36 mL|
References are publications that support the biological activity of the product.
Brough et al (2017) Application of off-rate screening in the identification of novel pan- isoform inhibitors of pyruvate dehydrogenase kinase. J.Med.Chem. 60 2271 PMID: 28199108
Moore et al (2014) 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 5 12862 PMID: 25404640
If you know of a relevant reference for VER 246608, please let us know.
Keywords: VER 246608, VER 246608 supplier, VER246608, pan-isoform, ATP, competitive, inhibitor, inhibits, pyruvate, dehydrogenase, kinase, PDK, PDHK, cancer, metabolism, tumor, microenvironment, Other, Kinases, 6604, Tocris Bioscience
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