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Merck
CN
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文件

安全信息

5.05766

Sigma-Aldrich

Casein Kinase II Inhibitor XII, TBBz

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别名:
Casein Kinase II Inhibitor XII, TBBz, 4,5,6,7-Tetrabromobenzimidazole, CYP24A1 inhibitor, TBBz, CK2 Inhibitor, TBBz
经验公式（希尔记法）:
C7H2Br4N2
CAS号:
577779-57-8
分子量:
433.72
MDL编号:
MFCD04116202
UNSPSC代码:
12352200

检测方案

≥99% (HPLC)

质量水平

100

形式

powder

效能

70 nM Ki

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

off-white

溶解性

DMSO: 100 mg/mL

储存温度

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

一般描述

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.

生化/生理作用

Primary Target
CK2
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

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.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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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, 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
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

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