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218697 Sigma-Aldrich

Casein Kinase II Inhibitor I - CAS 17374-26-4 - Calbiochem

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: Casein Kinase II Inhibitor I - CAS 17374-26-4 - Calbiochem, TBB, TBBt, 4,5,6,7-Tetrabromobenzotriazole, 4,5,6,7-Tetrabromo-2-azabenzimidazole, CK2 Inhibitor

  • CAS Number 17374-26-4

  • Empirical Formula (Hill Notation) C6HBr4N3

  • Molecular Weight 434.71

  •  MDL number MFCD06411399

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Properties

Related Categories A to C, Biochemicals and Reagents, Casein Kinase G, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme,
Quality Level   100
assay   ≥99% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   white
solubility   DMSO: 10 mg/mL
shipped in   ambient
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 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 µM, using rat liver and human recombinant CK2, respectively) and DYRK (IC50< 1 µM 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 µM, 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 (Cat. No. 218708) in DMSO, is also available.

Packaging

10 mg in Plastic ampoule

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.

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
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