PDK4-IN-1

PDK4-IN-1 is an anthraquinone-derived, orally active allosteric inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 of 84 nM. It binds to the lipoamide binding site of PDK4, preventing PDK4-mediated phosphorylation of the pyruvate dehydrogenase E1α subunit (PDHE1α). This promotes pyruvate dehydrogenase complex (PDC) activity, facilitating the conversion of pyruvate to acetyl-CoA and enhancing mitochondrial glucose oxidation. PDK4-IN-1 has demonstrated therapeutic potential in preclinical models of metabolic diseases (such as type 2 diabetes and insulin resistance), inflammatory conditions (such as acute-on-chronic liver failure and colitis), acute kidney injury, vascular smooth muscle cell proliferation (neointimal hyperplasia), and various cancers.

Other names

1-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)anthracene-9,10-dione1-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)anthracene-9,10-dione hydrochlorideCompound 8cCompound8cCompound-8cPDK4-IN-1 hydrochloridePDK-4-IN-1 hydrochloridePDK 4-IN-1 hydrochloride