DMAT

Solid. Soluble in DMSO (10mg/ml). Potent high affinity ATP-competitive inhibitor of casein kinase II (CK2) (IC50=0.13µM). Inhibits CK2 in rat liver with >1000-fold greater selectivity for CK2 than for CK1 (IC50=140nM and >200 &mu,M, respectively), DYRK1A and DYRK2 inhibitor (IC50= ~0.4µM for both), Shown to inhibit additional kinases, such as PIM1, PIM3, HIPK2, HIPK3, PKD1 and CDK2 in the submicromolar range, Anticancer agent. Apoptosis inducer in different cancer cell lines, Induces reactive oxygen species (ROS) and DNA double strand breaks in tumor cells, Induces apoptosis in cells expressing an inhibitor-resistant CK2, by inhibiting quinone reductase 2 (NQO2), binding with similar affinities to the oxidized and reduced forms of NQO2, Useful for in vivo studies due to cell permeability and high efficacy in cultured cells and implications in research and treatment of neoplasia and infective diseases, in which CK2 plays a role.