Biochem/physiol Actions
Primary TargetCDK2
Reversible: yes
Product competes with ATP.
Cell permeable: yes
Target IC50: 40 nM against CK2; 1.8, 2.1, 2.9, 3.5, 4.3, 7.5, 8.0, and 9.4 µM, against DNA topoisomerases I and II, Lyn, PKA catalytic subunit, Lyk, GSK-3, PKC, and FGR, respectively
General description
A cell-permeable, reversible, and potent antioxidant that has anti-mutagenic and anti-carcinogenic properties. Acts as a selective and ATP-competitive inhibitor of CK2 (IC50 = 40 nM). Moderately inhibits DNA topoisomerases I and II, Lyn, PKA catalytic subunit, Lyk, GSK-3, PKC, and FGR (IC50 = 1.8, 2.1, 2.9, 3.5, 4.3, 7.5, 8.0, and 9.4 µM, respectively). Only minimally inhibits DYRK1a, CSK, RET, Flt3, and NPM-ALK (IC50 >40 µM). Shown to act as an uncompetitive inhibitor of arginine methyltransferase CARM1 and block histone H3R17 methylation.
A cell-permeable, reversible, potent antioxidant that has anti-mutagenic and anti-carcinogenic properties. Acts as a selective and ATP-competitive inhibitor of CK2 (IC50 = 40 nM). Moderately inhibits DNA topoisomerases I and II, Lyn, PKA catalytic subunit, Lyk, GSK-3, PKC, and FGR (IC50 = 1.8, 2.1, 2.9, 3.5, 4.3, 7.5, 8.0, and 9.4 µM, respectively). Only minimally inhibits DYRK1a, CSK, RET, Flt3, and NPM-ALK (IC50 >40 µM). Shown to act as an uncompetitive inhibitor of arginine methyltransferase CARM1 and block histone H3R17 methylation.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Selvi, B.R., et al. 2009, J. Biol. Chem. In press.Cozza, G., et al. 2006. J. Med. Chem.49, 2363.Wang, B.H., et al. 1998. Planta Med. 64, 195.Constantinou, A., et al. 1995. Nutr. Cancer23, 121.Hickey, M.J., et al. 1995. Biochem. Soc. Trans.23, 607s.
Packaging
Packaged under inert gas
500 mg in Glass bottle
Preparation Note
For complete solubilization in ethanol, slight heating may be required.
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Ethanol stock solutions are stable for up to 1 week at -20°C. Alkaline solutions are unstable and should be prepared just prior to use.
Warning
Toxicity: Irritant (B)
This product has met the following criteria to qualify for the following awards: