Skip to Content
Merck
CN
All Photos(1)

Documents

Safety Information

5.05766

Sigma-Aldrich

Casein Kinase II Inhibitor XII, TBBz

Sign Into View Organizational & Contract Pricing
All Photos(1)
Synonym(s):
Casein Kinase II Inhibitor XII, TBBz, 4,5,6,7-Tetrabromobenzimidazole, CYP24A1 inhibitor, TBBz, CK2 Inhibitor, TBBz
Empirical Formula (Hill Notation):
C7H2Br4N2
CAS Number:
577779-57-8
Molecular Weight:
433.72
MDL number:
MFCD04116202
UNSPSC Code:
12352200

Assay

≥99% (HPLC)

Quality Level

100

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
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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

新产品

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

Piotr Zień et al.
Biochemical and biophysical research communications, 312(3), 623-628 (2003-12-19)
Two ATP-competitive inhibitors-4,5,6,7-tetrabromo-benzotriazole (TBBt) and 4,5,6,7-tetrabromo-benzimidazole (TBBz) have been shown to decrease activity of CK2 holoenzyme. Surprisingly it occurs that TBBz contrary to TBBt does not inhibit free catalytic subunit CK2 [Formula: see text]. Both inhibitors are virtually inactive against
Wei Luo et al.
Cancer research, 73(7), 2289-2297 (2013-01-30)
Vitamin D has broad range of physiological functions and antitumor effects. 24-Hydroxylase, encoded by the CYP24A1 gene, is the key enzyme for degrading many forms of vitamin D including the most active form, 1,25D(3). Inhibition of CYP24A1 enhances 1,25D(3) antitumor
Piotr Zień et al.
Biochemical and biophysical research communications, 306(1), 129-133 (2003-06-06)
Like the previously reported 4,5,6,7-tetrabromobenzotriazole (TBBt), the structurally related 4,5,6,7-tetrabromobenzimidazole (TBBz) is a selective ATP-competitive inhibitor of protein kinase CK2 from such divergent sources as yeast, rat liver, Neurospora crassa and Candida tropicalis, with K(i) values in the range 0.5-1
Piotr Zien et al.
Biochimica et biophysica acta, 1754(1-2), 271-280 (2005-10-06)
The development of selective cell-permeable inhibitors of protein kinase CK2 has represented an important advance in the field. However, it is important to not overlook the existence of discrete molecular forms of CK2 that arise from the presence of distinct
R Szyszka et al.
Biochemical and biophysical research communications, 208(1), 418-424 (1995-03-08)
Several halogeno benzimidazole riboside inhibitors of animal and plant protein kinases CK I and CK II (also known as casein kinases I and II), were found to be effective inhibitors of Saccharomyces cerevisiae CK II, but not of the 27-kDa

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service