General description
A cell-permeable α-cyanocinnamate compound that acts as a rapid, active site thiol modifying, time-dependent and non-competitive inhibitor of bi-directional pyruvate transport across plasma membranes in yeast, bacteria, Drosophila, and humans (IC50 = 50 nM in rat heart mitochondria; Ki ≤ 1 µM) with excellent selectivity over monocarboxylates and anions. Shown to significantly decrease pyruvate-driven respiration, enhance glucose uptake and activate AMPK (2 µM in human myocytes and skeletal muscle myotubes).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
mitochondria
Reversible: no
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C or -70°C). Stock solutions are stable for up to 2 weeks at -20°C or for up to 6 weeks at -70°C.
Use only fresh DMSO for reconstitution.
Other Notes
Divakaruni, A.S., et al. 2013. Proc. Natl. acad. Sci. USA110, 5422.
Bricker, D.K., et al. 2012. Science337, 96.
Herzig, S., et al. 2012. Science337, 93.
Hinoi, E., et al. 2006. Mol. Pharmacol.70, 925.
Hildyard, J.C.W., et al. 2005. Biochim. Biophys. Acta1707, 221.
Halestrap, A.P. 1978. Biochem. J.172, 377.
Halestrap, A.P. 1975. Biochem. J.145, 85.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51281514
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5048170001
