PS10

PS10 is a small molecule inhibitor of the pyruvate dehydrogenase kinase (PDK) family, with high potency and selectivity for the PDK2 and PDK4 isoforms. By inhibiting PDK, PS10 prevents the phosphorylation and subsequent inactivation of the pyruvate dehydrogenase complex (PDC), thereby promoting the conversion of pyruvate into acetyl-CoA for entry into the tricarboxylic acid (TCA) cycle. This metabolic shift reverses the Warburg effect (aerobic glycolysis) commonly observed in cancer cells, leading to reduced tumor cell proliferation and enhanced sensitivity to chemotherapeutic agents such as cisplatin. Preclinical research has demonstrated its efficacy in bladder cancer models and suggested potential applications in metabolic disorders like type 2 diabetes by improving glucose oxidation.

Other names

2-[(2,4-dihydroxyphenyl)sulfonyl]isoindoline-5-carboxamide