UK-5099

- Overview
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    Background
    
    UK-5099 is a potent inhibitor of the mitochondrial pyruvate carrier [1]. The mitochondrial pyruvate carrier (MPC) facilitates pyruvate transport across the mitochondrial inner membrane and plays a critical role in carbohydrate, lipid and amino acid metabolism.UK-5099 (1 mM) completely blocked pyruvate uptake with Ki value of 49 μM. Also, UK-5099 decreased the overall efflux rate in a concentration-dependant way [1]. In mitochondria isolated from S. Guttatum, UK-5099 (20 μM) inhibited pyruvate-dependent 02 consumption [2]. In rat heart mitochondria, UK-5099 inhibited pyruvate oxidation with a non-linear inhibition kinetics [2]. In glucagon-treated rats, UK-5099 inhibited pyruvate carboxylation and total pyruvate metabolism with a linear relationship [3]. In rat liver and heart mitochondria, UK-5099 inhibited pyruvate-dependent 02 consumption with IC50 value of 50 nM [4].
    
    [1]. Wiemer EA, Michels PA, Opperdoes FR. The inhibition of pyruvate transport across the plasma membrane of the bloodstream form of Trypanosoma brucei and its metabolic implications. Biochem J, 1995, 312 ( Pt 2): 479-484.
    [2]. Halestrap AP. The mitochondrial pyruvate carrier. Kinetics and specificity for substrates and inhibitors. Biochem J, 1975, 148(1): 85-96.
    [3]. Halestrap AP, Armston AE. A re-evaluation of the role of mitochondrial pyruvate transport in the hormonal control of rat liver mitochondrial pyruvate metabolism. Biochem J, 1984, 223(3): 677-685.
    [4]. Proudlove MO, Beechey RB, Moore AL. Pyruvate transport by thermogenic-tissue mitochondria. Biochem J, 1987, 247(2): 441-447.
- Properties
  - Alternative Name
    
    PF-1005023;UK5099;UK 5099;PF1005023;PF 1005023; (E)-2-cyano-3-(1-phenylindol-3-yl)prop-2-enoic acid
    
    CAS Number
    
    56396-35-1
    
    Molecular Formula
    
    C18H12N2O2
    
    Molecular Weight
    
    288.3
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥28.8 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Li A, Liu Q, et al. "Berberine Reduces Pyruvate-driven Hepatic Glucose Production by Limiting Mitochondrial Import of Pyruvate through Mitochondrial Pyruvate Carrier 1." EBioMedicine. 2018 Aug;34:243-255. PMID:30093307

UK-5099

Background

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