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Sigma-Aldrich

Casein Kinase II Inhibitor I

The Casein Kinase II Inhibitor I, also referenced under CAS 17374-26-4, controls the biological activity of Casein Kinase II. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

Casein Kinase II Inhibitor I, TBB, TBBt, 4,5,6,7-Tetrabromobenzotriazole, 4,5,6,7-Tetrabromo-2-azabenzimidazole, CK2 Inhibitor

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About This Item

Empirical Formula (Hill Notation):
C6HBr4N3
CAS Number:
17374-26-4
Molecular Weight:
434.71
MDL number:
MFCD06411399
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥99% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 10 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C6HBr4N3/c7-1-2(8)4(10)6-5(3(1)9)11-13-12-6/h(H,11,12,13)

InChI key

OMZYUVOATZSGJY-UHFFFAOYSA-N

General description

A cell-permeable benzotriazolo compound that acts as a highly selective, ATP/GTP-competitive casein kinase II (CKII) inhibitor (IC50 = 900 nM and 1.6 µM for rat liver and human recombinant CKII, respectively) and DYRK (IC50<1 µM for DYRK1a). Specificity for CKII has been reported following the screening of 33 kinases, including PKA, Akt, PKC, MKK1, ERK2, p38, JNK, Lck, Lyn, and Syk. Also reported to inhibit NS3-associated viral helicase activity in hepatitis C virus (HCV) (IC50 = 20 and 60 µM using DNA and RNA substrates, respectively) and West Nile virus (WNV) (IC50 = 1.7 µM and 900 nM using DNA and RNA substrates, respectively).
A cell-permeable benzotriazolo compound that acts as a higly selective, reversible, and ATP/GTP-competitive inhibitor of casein kinase-2 (CK2) (IC50 = 900 nM and 1.6 M, using rat liver and human recombinant CK2, respectively) and DYRK (IC50<1 M for DYRK1a). Its specificity has been demonstrated using a panel of 33 kinases, including PKA, PKB, PKC, MKK1, Erk2, p38, JNK, Lck, Lyn, and Syk. Also shown to inhibit NS3-associated viral helicase activities in HCV (IC50 = 20 and 60 M, using DNA and RNA substrate, respectively) and WNV (IC50 = 1.7 and 900 nM, using DNA and RNA substrate, respectively). A 10 mM (5 mg/1.15 ml) solution of Casein Kinase II Inhibitor I in DMSO, is also available.

Biochem/physiol Actions

Cell permeable: yes
Product competes with ATP.
Reversible: yes
Target IC50: 900 nM and 1.6 µM, using rat liver and human recombinant CK2, respectively; <1 µM for DYRK1a

Packaging

Packaged under inert gas

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Other Notes

Borowski, P., et al. 2003. Eur. J. Biochem.270, 1645.
Sarno, S., et al. 2003. Biochem. J.374, 639.
Zien, P., et al. 2003. Biochem. Biophys. Res. Commun.306, 129.
Ruzzene, M., et al. 2002. Biochem. J.364, 41.
Sarno, S., et al. 2001. FEBS Lett.496, 44.
Szyszka, R., et al. 1995. Biochem. Biophys. Res. Commun.208, 418.

Legal Information

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

wgk_germany

WGK 3

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