Biological Activity
UK-5099 is a potent inhibitor of the mitochondrial pyruvate carrier (MPC). UK-5099 ihibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.
In Vitro
The trypanosomal pyruvate carrier is found to be rather insensitive to inhibition by alpha-cyano-4-hydroxycinnamate (Ki=17 mM) but can be completely blocked by UK-5099 (Ki=49 microM)[2]. UK-5099 also inhibits the monocarboxylate transporter (MCT) [3]. UK5099 significantly inhibits the glucose-stimulated rise in oxygen consumption in a dose-dependent manner and at 150 μM reduced oxygen consumption below basal levels. UK5099 reduces ATP levels and increases ADP and AMP levels in 832/13 cells[4]. The UK5099 treated cells show significantly higher proportion of side population fraction and express higher levels of stemness markers Oct3/4 and Nanog. UK5099 application may be an ideal model for Warburg effect studies[5].
In Vivo
The MPC inhibitor UK5099 increases the glucose excursion seen during an intraperitoneal glucose tolerance test in C57BLK mice[4].
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.