UK-5099 is a potent is MPC (mitochondrial pyruvate carrier) inhibitor with IC50 value of 50 nM.
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HazMat fee for 500 gram (Estimated)
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The mitochondrial pyruvate carriers (MPC) mediate pyruvate import into the mitochondria, which is key to the sustenance of the tricarboxylic cycle and oxidative phosphorylation[3]. In two distinct CRC mouse models, loss of Mpc1 prior to a tumorigenic stimulus doubled the frequency of adenoma formation and produced higher grade tumors. MPC loss was associated with a glycolytic metabolic phenotype and increased expression of stem cell markers. UK-5099 (PF-1005023) is a potent inhibitor of MPC[4]. UK-5099 (PF-1005023) inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.[5]. 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 mM)[6]. UK-5099 also inhibits the monocarboxylate transporter (MCT)[7]. 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[8]. 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[9].
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