PDHK1 (human, recombinant)

Pyruvate dehydrogenase kinase 1 (PDHK1) is a kinase and regulator of glycolysis and oxidative phosphorylation.^1,2,3 It is expressed primarily in the heart and to a lesser extent in skeletal muscle, liver, brain, placenta, lung, pancreas, and kidney and is localized to the mitochondria.¹ PDHK1 phosphorylates three serine residues on the E1 subunit of the pyruvate dehydrogenase complex, inhibiting the oxidative decarboxylation of pyruvate to acetyl-CoA and instead promoting its conversion to lactate.^2,3 Pharmacologic inhibition of PDHK1 inhibits both proliferation and survival of T helper 17 (Th17) cells and suppresses Th17-mediated inflammation in rodent models of inflammatory bowel disease (IBD) and experimental autoimmune encephalomyelitis (EAE).² Levels of PDHK1 are increased in and associated with malignancy in lung cancers and pancreatic ductal adenocarcinomas, and pharmacologic inhibition of PDHK1 reverses the Warburg phenotype in various tumor models in vitro and in vivo.^4,3 Cayman’s PDHK1 (human, recombinant) protein can be used for activity assay, binding study, and Western blot (WB) applications.

WARNING This product is not for human or veterinary use.

1. Gudi, R., Bowker-Kinley, M.M., Kedishvili, N.Y., et al. Diversity of the pyruvate dehydrogenase kinase gene family in humans. The Journal of Biological Chemisty 270(48), 28989-28994 (1995).

2. Gerriets, V.A., Kishton, R.J., Nichols, A.G., et al. Metabolic programming and PDHK1 control CD4⁺ T cell subsets and inflammation. J. Clin. Invest. 125(1), 194-207 (2015).

3. Xu, H., Ding, D., Han, X., et al. Discovery of ATP competitive PDHK1/2 dual inhibitors. Bioorg. Med. Chem. Lett. 122, 130190 (2025).

4. Wu, P., Zhang, Z., Zhou, Y., et al. Novel dichloroacetophenone-based PDHK1 inhibitors as potent anticancer agents. Drug Des. Devel. Ther. 18, 4661-4679 (2024).