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 p72syk (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 p72syk (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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Activity of rat liver protein kinase A catalytic subunit
Product competes with ATP.
Reversible: yes
Target IC50: 3 µM, 8 µM, and 12 µM against the activity of rat liver protein kinase A catalytic subunit, PKC, and MLCK, respectively
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 41116113
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 527948-1MG