Casein Kinase II Inhibitor I

Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Cell permeable: yes

Target IC₅₀: 900 nM and 1.6 µM, using rat liver and human recombinant CK2, respectively; ﹤1 µM for DYRK1a

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.

Legal Information

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

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.

Packaging

Packaged under inert gas

10 mg in Plastic ampoule

Warning

Toxicity: Carcinogenic / Teratogenic (D)