VER 246608

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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% (HPLC)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity for VER 246608

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 for VER 246608

M. Wt 552.96
Formula C28H23ClF2N4O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1684386-71-7
PubChem ID 86280454
InChI Key LCGNLQSOSJFLKR-UHFFFAOYSA-N
Smiles O=C(C1=CC=C(O)C=C1O)N(C=2C=CC(=CC2)C3=NC(Cl)=NC=C3C)CC4=CC=C(C=C4)CNC(=O)C(F)F

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.

Solubility Data for VER 246608

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 55.3 100

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for VER 246608

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


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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

Citations for VER 246608

Citations are publications that use Tocris products.

Currently there are no citations for VER 246608. Do you know of a great paper that uses VER 246608 from Tocris? Please let us know.

Reviews for VER 246608

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Literature in this Area

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Cancer Research Product Guide

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases Product Listing

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases