For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>UK-5099(PF1005023) is a potent inhibitor of plasma membrane monocarboxylate transporters (MCTs) and the mitochondrial pyruvate carrier (MPC); inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.<br>IC50 value: 50 nM<br>Target: MCT<br>The trypanosomal pyruvate carrier was found to be rather insensitive to inhibition by alpha-cyano-4-hydroxycinnamate (Ki = 17 mM) but could be completely blocked by UK5099 (Ki = 49 microM). Inhibition of pyruvate transport resulted in the retention, and concomitant accumulation, of pyruvate within the trypanosomes, causing acidification of the cytosol and osmotic destabilization of the cells. UK-5099 is more powerful inhibitor than alpha-cyano-4-hydroxycinnamate showing 50% inhibition of pyruvate-dependent O2 consumption by rat heart mitochondria at concentrations of 200, 200 and 50 nM respectively.</p>
| Catalog Number | I004108 |
| CAS Number | 56396-35-1 |
| Synonyms | (E)-2-cyano-3-(1-phenylindol-3-yl)prop-2-enoic acid |
| Molecular Formula | C₁₈H₁₂N₂O₂ |
| Purity | ≥95% |
| Target | Mitochondrial Metabolism |
| Solubility | DMSO >20 mg/mL |
| Storage | Store at -20°C |
| IC50 | 50 nM |
| 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-JLHYYAGUSA-N |
| SMILES | C1=CC=C(C=C1)N2C=C(C3=CC=CC=C32)C=C(C#N)C(=O)O |
| Reference | <p style=/line-height:25px/> |
