Casein Kinase II Inhibitor VIII

Biochem/physiol Actions

Primary TargetCK2

Target IC₅₀: 32 and 46 nM for CK2&alpha

Secondary TargetDYRK1B, Flt-3

Reversible: yes

Cell permeable: yes

General description

A cell-permeable thiazolamide compound that acts as a potent, reversible, and ATP-competitive inhibitor against casein kinase-2/CK2 (IC₅₀ = 32 and 46 nM against CK2α and CK2α′, respectively), as well as DYRK1B and FLt-3 (82% and 76% inhibition, respectively, at 30 nM), while diplaying reduced or little potency toward other targets in a 70-kinase panel selectivity profile study. Shown to effectively block the proliferation of a variety of cancer cells (IC₅₀ = 2.6, 1.6, and 2.4 µM, in A549, HCT116, and MCF-7 cultures, respectively).

Legal Information

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

Other Notes

Hou, Z., et al. 2012. J. Med. Chem.55, 2899.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)