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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
CDK2
Product competes with ATP.
Reversible: 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
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51131752
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 324683-500MG