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Description: MCT inhibitor; also inhibits mitochondrial pyruvate carrier
Chemical Name: 2-Cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoic acid
Purity: ≥98% (HPLC)
Biological Activity for UK 5099
UK 5099 is an inhibitor of plasma membrane monocarboxylate transporters (MCTs) and the mitochondrial pyruvate carrier (MPC).
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for UK 5099
UK 5099 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for UK 5099
| M. Wt | 288.3 |
| Formula | C18H12N2O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 56396-35-1 |
| PubChem ID | 6438504 |
| InChI Key | BIZNHCWFGNKBBZ-JLHYYAGUSA-N |
| Smiles | O=C(/C(C#N)=C/C2=CN(C3=CC=CC=C3)C1=CC=CC=C12)O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for UK 5099
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 28.83 | 100 |
Preparing Stock Solutions for UK 5099
The following data is based on the product molecular weight 288.3. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.47 mL | 17.34 mL | 34.69 mL |
| 5 mM | 0.69 mL | 3.47 mL | 6.94 mL |
| 10 mM | 0.35 mL | 1.73 mL | 3.47 mL |
| 50 mM | 0.07 mL | 0.35 mL | 0.69 mL |
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Product Datasheets for UK 5099
References for UK 5099
References are publications that support the biological activity of the product.
Wiemer et al (1995) The inhibition of pyruvate transport across the plasma membrane of the bloodstream form of Trypanosoma brucei and its metabolic implications. Biochem.J. 312 479 PMID: 8526859
Hildyard et al (2003) Identification of the mitochondrial pyruvate carrier in Saccharomyces cerevisiae. Biochem.J. 374 607 PMID: 12887330
Hinoi et al (2006) A molecular mechanism of pyruvate protection against cytotoxicity of reactive oxygen species in osteoblasts. Mol.Pharmacol. 70 925 PMID: 16766717
If you know of a relevant reference for UK 5099, please let us know.
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Keywords: UK 5099, UK 5099 supplier, UK5099, inhibitor, transporters, mitochondrial, pyruvate, transport, carriers, inhibitors, MPT, inhibits, monocarboxylate, transporter, MCT, Monocarboxylate, Transporters, 4186, Tocris Bioscience
7 Citations for UK 5099
Citations are publications that use Tocris products. Selected citations for UK 5099 include:
Tompkins et al (2019) Disrupting Mitochondrial Pyruvate Uptake Directs Glutamine into the TCA Cycle away from Glutathione Synthesis and Impairs Hepatocellular Tumorigenesis. Cell Rep 28 2608 PMID: 31484072
Lei et al (2019) Metabolic Control of Astrocyte Pathogenic Activity via cPLA2-MAVS. Cell 179 1483-1498.e22 PMID: 31813625
Oliver J et al (2022) A non-canonical tricarboxylic acid cycle underlies cellular identity. Nature 603 477-481 PMID: 35264789
Keit Men et al (2020) A glycolytic shift in Schwann cells supports injured axons. Nat Neurosci 23 1215-1228 PMID: 32807950
Rauckhorst et al (2017) The mitochondrial pyruvate carrier mediates high fat diet-induced increases in hepatic TCA cycle capacity. Mol Metab 6 1468 PMID: 29107293
Kaji et al (2015) SCFA transport in rat duodenum. Nat Chem Biol 308 G188 PMID: 25394661
Santosh et al (2021) The mitochondrial carrier SFXN1 is critical for complex III integrity and cellular metabolism. Cell Rep 34 108869 PMID: 33730581
Do you know of a great paper that uses UK 5099 from Tocris? Please let us know.
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