pdk4-in-1

PDK4-IN-1, an anthraquinone derivative, is a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 value of 84 nM.

PDK4-IN-1 hydrochloride, an anthraquinone derivative, is a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 value of 84 nM.

PDK-IN-2 (Compound 1F), with an IC50 of 68 nM, is a potent PDK inhibitor that downregulates the expression of PDK1 and PDK4 in cells. It promotes mitochondrial bioenergetics, reduces glycolytic activity, and triggers apoptosis via the mitochondrial pathway. Additionally, PDK-IN-2 has been shown to impede tumor growth in a 4T1 syngeneic mouse model [1].

PDK4-IN-2 (compound 8), a pyruvate dehydrogenase kinase 4 (PDK4) inhibitor, exhibits an inhibition concentration (IC 50) of 46 µM. By regulating bioenergetics and activating the tricarboxylic acid cycle [1], it enhances the ejection fraction in failing hearts.