5.05766
Casein Kinase II Inhibitor XII, TBBz
Synonym(s):
Casein Kinase II Inhibitor XII, TBBz, 4,5,6,7-Tetrabromobenzimidazole, CYP24A1 inhibitor, TBBz, CK2 Inhibitor, TBBz
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About This Item
Empirical Formula (Hill Notation):
C7H2Br4N2
CAS Number:
Molecular Weight:
433.72
UNSPSC Code:
12352200
MDL number:
Assay:
≥99% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
assay
≥99% (HPLC)
Quality Segment
form
powder
potency
70 nM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 100 mg/mL
storage temp.
2-8°C
InChI
1S/C7H2Br4N2/c8-2-3(9)5(11)7-6(4(2)10)12-1-13-7/h1H,(H,12,13)
InChI key
LOEIRDBRYBHAJB-UHFFFAOYSA-N
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
CK2
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
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.
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
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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