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.

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

Packaged under inert gas

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.

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

Toxicity: Carcinogenic / Teratogenic (D)