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In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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].References:[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.
Cell lines
832/13 cells derived from INS-1 rat insulinoma cells
Reaction Conditions
50 ~ 150 μM UK-5099 for 30 ~ 65 min incubation
Applications
UK-5099 significantly inhibited the glucose-stimulated rise in oxygen consumption in a dose-dependent manner and at 150 μM reduced oxygen consumption below basal levels. Moreover, UK-5099 (150 μM) reduced ATP levels and increased ADP and AMP levels in 832/13 cells.
Animal models
C57BLK mice
Dosage form
32 μmol/kg
Injected intraperitoneally 30 min before the glucose challenge
UK-5099 caused a significantly greater glucose excursion at 30, 60, and 120 min as compared with DMSO control mice. The area under the curve was also significantly increased by UK-5099 as compared with DMSO control mice. Thus, UK-5099 resulted in impaired glucose tolerance in vivo.
Note
The technical data provided above is for reference only.
References:
1. Patterson JN, Cousteils K, Lou JW, et al Mitochondrial metabolism of pyruvate is essential for regulating glucose-stimulated insulin secretion. Journal of Biological Chemistry, 2014, 289(19): 13335-13346.
