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AB668

Chemical Structure : AB668

CAS No.: 2757727-52-7

AB668 (AB 668, AB-668)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 638.80
Formula C33H43FN6O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

isobutyl 5-fluoro-3-(1-((1-(2-((4-isobutylphenyl)sulfonamido)ethyl)piperidin-4-yl)methyl)-1H-1,2,3-triazol-4-yl)-1H-indole-2-carboxylate

References

1. Alexandre Bancet, et al. iScience. 2024 Jan 12;27(2):108903.

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