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Background: Pyruvate dehydrogenase kinase (PDK) has 4 isoforms: PDK1, PDK2, PDK3, and PDK4. PDKs regulate the metabolic link between glycolysis and the TCA (tricarboxylic acid) cycle. PDK activity is inhibited by phosphorylation of serine residues on PDH (pyruvate dehydrogenase). Each isoform is expressed differently across different tissues types, and their activity is affected by cell energy availability and insulin levels. PDK1-3 have been found to act as oncogenes, their expression linked to higher rates of tumor metastasis and proliferation. However, upregulation of PDK4 may act as a tumor suppressor in lung cancer and hepatocellular carcinoma (HCCa) cells. PDK inhibitors have been developed to target diabetes, cancer, and heart disease.
CAS Number: 1684386-71-7
Description: VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.1
Format: Solid.
Purity: ≥90%
Storage Stability: Powder, store up to 3 years at -20°C or up to 2 years at 4°C. In solvent, store up to 2 years at -80°C or up to 1 year at -20°C
Target: PDK1, PDK2, PDK3, PDK4
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Moore JD, et al., 2014 Oncotarget 5(24): 12862-76.
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