VER-246608

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

Product Specifications

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

Purity

≥ 90%

Format

Solid.

Solubility

Soluble in DMSO up to 100 mg/mL.

Molecular Formula

C28H23ClF2N4O4

Shipping Conditions

Room Temperature

Storage Conditions

Powder-20°C3 years4°C2 yearsIn solvent-80°C2 years-20°C1 year

Calculated Molecular Weight

552.96 Da