General description
A cell-permeable halogenated benzimidazole compound that acts as a selective and ATP competitive inhibitor of casein kinase II (CK2, Ki = 70 nM for the active hetero-tetrameric form). However, its effect on free CK2a and CK2a′ subunits is significantly reduced (Ki = 510 and 400 nM, respectively). Reported to reduce viability and proliferation in HeLa, Jurkat, and HL-60 cells (at ˜25 µM). Also shown to disrupt the promoter activity of CYP24A1 and down-regulates its endogenous and 1, 25-Vitamin D3 (1,25-D3)-induced expression in PC3 cells. Synergistically enhances the anti-tumor effect of 1, 25-D3 in a PC3 xenograft murine model.
Biochem/physiol Actions
Primary Target
CK2
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Szyszka, R. et al. 1995. Biochem. Biophys. Res. Comm.208, 418.
Zien, P. et al. 2003. Biochem. Biophys. Res. Comm.306, 129.
Zien, P. et al. 2003. Biochem. Biophys. Res. Comm.312, 623.
Zien, P. et al. 2005. Biochim. Biophy. Acta1754, 271.
Luo, W. et al. 2013. Cancer Res.73, 2289.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5057660001
