UK-5099

Research use only, not for human use.

UK 5099 is a specific and potent inhibitor of MPC carrier activity. It potently inhibits pyruvate-dependent oxygen consumption by rat heart mitochondria (IC50: 50 nM).

UK-5099 is a specific and potent mitochondrial pyruvate carrier blocker (MCK blocker). The UK5099 treated cells showed significantly higher proportion of side population (SP) fraction and expressed higher levels of stemness markers Oct3/4 and Nanog. Chemosensitivity examinations revealed that the UK5099 treated cells became more resistant to chemotherapy compared to the non-treated cells. MPC blocker (UK5099) application may be an ideal model for Warburg effect studies(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). UK-5099 also inhibits the monocarboxylate transporter (MCT) . 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. 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.(In Vivo):The MPC inhibitor UK5099 increases the glucose excursion seen during an intraperitoneal glucose tolerance test in C57BLK mice.

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UK-5099, UK 5099, UK5099

Others

Other Targets

MPC

Cancer

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56396-35-1

288.3

C18H12N2O2

>98% (HPLC)

DMSO : ≥ 50 mg/mL. 173.43 mM; H2O : < 0.1 mg/mL

OC(=O)C(=Cc1cn(-c2ccccc2)c2ccccc12)C#N

2-cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoic acid

(-20℃)

With Ice Pack

≥ 2 years