AB668 is a selective, bivalent Casein Kinase 2 (CK2) inhibitor targeting the ATP site and the αD pocket, AB668 inhibits the CK2 holoenzyme with Ki value of 41 nM (IC50=65 nM).
AB668 inhibits the phosphorylation of a CK2 protein substrate SIX1 bout 90% in the presence of 0.5 uM.
AB668 shows high affinity with KD of 86 nM for CK2α in KINOMEscan profiling assay (Eurofins).
AB668 displays an outstanding selectivity against a large kinase panel at 2 uM.
AB668 induces apoptotic cell death in cancer cells, induces caspase-3 activation and reduces the expression of survivin, exhibits a broad effect on cell death in various cancer cells.
AB668 demonstrates target engagement in HEK293 cells with IC50 values of 0.34 and 0.60 μM for 786-O cells and HEK293 cells, respectively.
AB668 induces a deep alteration of antiapoptotic pathways, cell cycle and mitotic processes, as well as steroids and lipids metabolism, compared to pure ATP-competitive CX-4945 inhibitor.