218697

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
• Empirical Formula (Hill Notation): C₆HBr₄N₃
• CAS Number: 17374-26-4
• Molecular Weight: 434.71
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD06411399
• Assay: ≥99% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Quality Segment: 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
• SMILES string: Brc1c2n[nH]nc2c(c(c1Br)Br)Br
• 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

Description

General description

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

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

Disclaimer

Toxicity: Carcinogenic / Teratogenic (D)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3