PDK-IN-3 (compound 1) is a potent pan inhibitor of PDK with IC50s of 109.3, 135.8, 458.7 nM and 8.67 μM against PDK 1-4, respectively. PDK-IN-3 also induces proliferation and apoptosis in A549 cells.
References:
[1]. Gan L, et al. Targeting the pyruvate dedrogenase complex/pyruvate dedrogenase kinase (PDC/PDK) axis to discover potent PDK inhibitors through structure-based virtual screening and pharmacological evaluation. Eur J Med Chem. 2023 Dec 3;264:116008.