Chemical Structure : AB668
货号: PC-21783Not For Human Use, Lab Use Only.
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).
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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.
分子量 | 638.80 | |
分子式 | C33H43FN6O4S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Alexandre Bancet, et al. iScience. 2024 Jan 12;27(2):108903.
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