Biochem/physiol Actions

Reversible: no

Cell permeable: yes

Primary Targetmitochondria

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; K_i ≤ 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).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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.

Packaging

5 mg in Glass bottle

Packaged under inert gas

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.

Warning

Toxicity: Standard Handling (A)