JX06

JX06 is a **potent and selective small molecule inhibitor of pyruvate dehydrogenase kinase 1 (PDK1)**, with additional activity against PDK2 and PDK3 at higher concentrations. It selectively forms a covalent disulfide bond with a conserved cysteine (C240) in PDK1, leading to enzyme inactivation and inhibition of glycolysis, especially in cancer cells that rely heavily on glycolytic metabolism. JX06 shows anti-proliferative effects in vitro in A549 human lung cancer and multiple myeloma cells, induces apoptosis in cancer cells, reduces tumor volume in A549 xenograft models, and exhibits synergy in combination with other agents such as metformin or bortezomib. Its use has also been explored in endometrial cancer models with metabolic comorbidities and as a nanoparticle formulation for targeted delivery. JX06 is a research tool and is not approved for clinical use.

Other names

Bis(morpholinothiocarbonyl) disulfide