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UK 5099
- PF 1005023
Axon 2805
CAS:
56396-35-1
Purity:
99%
- Soluble in DMSO
- MF: C18H12N2O2
- MW: 288.3
Description
UK 5099 is a potent inhibitor of the mitochondrial pyruvate carrier (MPC), preventing transport of cytosolic pyruvate into the mitochondrial matrix. At low concentrations, it is commonly used to acutely suppress pyruvate-supported mitochondrial respiration and oxidation.
UK 5099 can also inhibit plasma-membrane monocarboxylate transporters (MCTs) at substantially higher concentrations, so dose selection is important when assigning metabolic effects specifically to MPC blockade. It is used in flux analysis, substrate-utilization studies and models of metabolic flexibility.
Key Features
- Potent MPC inhibitor
- Blocks mitochondrial pyruvate uptake
- Suppresses pyruvate-supported respiration
- Can inhibit MCTs at higher concentrations
Applications
- MPC1/MPC2 research
- Mitochondrial fuel-selection studies
- Metabolic flux analysis
- Glycolysis–oxidation coupling research
- Cellular metabolic-flexibility assays
More Information
| Parent CAS No. | 56396-35-1 |
|---|---|
| Chemical Name | 2-Cyano-3-(1-phenyl-1H-indol-3-yl)acrylic acid |
| extra_info | Thiolox |
| SMILES | C1C(N2C3C=CC=CC=3C(/C=C(C(O)=O)/C#N)=C2)=CC=CC=1 |
| MFCD | MFCD19443867 |
| InChi | InChI=1S/C18H12N2O2/c19-11-13(18(21)22)10-14-12-20(15-6-2-1-3-7-15)17-9-5-4-8-16(14)17/h1-10,12H,(H,21,22)/b13-10- |
| InChiKey | BIZNHCWFGNKBBZ-RAXLEYEMSA-N |
| CID | 20839118 |
| Short Description | MPC inhibitor |
UK 5099
potent MPC inhibitor
PF 1005023
UK5099
UK-5099
PF1005023
PF-1005023
Pyruvate
MPC
Inhibitor
MPC1/MPC2 research
Mitochondrial fuel-selection studies
Metabolic flux analysis
Glycolysis–oxidation coupling research
Cellular metabolic-flexibility assays
mitochondrial function
metabolism
enzyme pharmacology
drug discovery
CAS 56396-35-1
Axon Medchem
Axon 2805
Supplier
Vendor
References
- MS Shearman et al. The concentration of the mitochondrial pyruvate carrier in rat liver and heart mitochondria determined with alpha-cyano-beta-(1-phenylindol-3-yl)acrylate. Biochem J. 1984 Nov 1;223(3):673-6.
- JC Hildyard et al. Identification and characterisation of a new class of highly specific and potent inhibitors of the mitochondrial pyruvate carrier. Biochim Biophys Acta. 2005 Apr-May;1707(2-3):221-30.
- Y Zhong et al. Application of mitochondrial pyruvate carrier blocker UK5099 creates metabolic reprogram and greater stem-like properties in LnCap prostate cancer cells in vitro. Oncotarget. 2015 Nov 10;6(35):37758-69.
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