Piceatannol

Biochem/physiol Actions

Primary TargetActivity of rat liver protein kinase A catalytic subunit

Reversible: yes

Product competes with ATP.

Target IC₅₀: 3 µM, 8 µM, and 12 µM against the activity of rat liver protein kinase A catalytic subunit, PKC, and MLCK, respectively

Cell permeable: yes

General description

A cell-permeable, substrate competitive and reversible plant metabolite that inhibits the activity of rat liver protein kinase A catalytic subunit (IC₅₀ = 3 µM), PKC (IC₅₀ = 8 µM), MLCK (IC₅₀ = 12 µM). In RBL-2H3 cells, the selective inhibition of Syk by piceatannol results in inhibition of FceR1-mediated signaling. Also inhibits wheat embryo Ca²⁺-dependent protein kinase (CDPK) (IC₅₀ = 19 µM), and p72^syk (IC₅₀ = 10 µM), a non-receptor tyrosine kinase, relative to Lyn in isolated enzyme preparations. Also possesses anti-leukemic properties. Reported to activate sirtuins and promote the survival of eukaryotic cells.

A cell-permeable, substrate competitive, and reversible plant metabolite that inhibits the activity of rat liver protein kinase A catalytic subunit (IC₅₀ = 3 µM), PKC (IC₅₀ = 8 µM), MLCK (IC₅₀ = 12 µM). In RBL-2H3 cells, the selective inhibition of Syk by piceatannol results in inhibition of FceR1-mediated signaling. Also inhibits wheat embryo Ca²⁺-dependent protein kinase (CDPK) (IC₅₀ = 19 µM), and p72^syk (IC₅₀ = 10 µM), a non-receptor tyrosine kinase, relative to Lyn in isolated enzyme preparations. Also possesses anti-leukemic properties. Reported to activate sirtuins and promote the survival of eukaryotic cells.

Legal Information

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

Other Notes

Howitz, K.T., et al. 2003. Nature425, 191.Wang, B.H., et al. 1998. Planta Med. 64, 195.Keely, P.J., and Parise, L.V. 1996. J. Biol. Chem. 271, 26668.Oliver, J.M., et al. 1994. J. Biol. Chem. 269, 29697.Thakkar, K., et al. 1993. J. Med. Chem. 36, 2950.Geahlen, R.L., et al. 1989. Biochem. Biophys. Res. Commun. 165, 241.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot, flush with an inert gas, and freeze (-20°C). Stock solutions are stable for up to 2 weeks at -20°C.

Warning

Toxicity: Standard Handling (A)