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Benzimidazole Inhibitors of Protein Kinase CK2 Potently Inhibit the Activity of Atypical Protein Kinase Rio1

Benzimidazole Inhibitors of Protein Kinase CK2 Potently Inhibit the Activity of Atypical Protein Kinase Rio1

Konrad Kubiński, Maciej Masłyk, Andrzej Orzeszko

Mol Cell Biochem. 2017 Feb;426(1-2):195-203.

PMID: 27909846

Abstract:

Benzimidazole derivatives of 5,6-dichlorobenzimidazole 1-β-D-ribofuranoside (DRB) comprise the important class of protein kinase CK2 inhibitors. Depending on the structure, benzimidazoles inhibit CK2 with different selectivity and potency. Besides CK2, the compounds can inhibit, with similar activity, other classical eukaryotic protein kinases (e.g. PIM, DYRK, and PKD). The present results show that a majority of the most common CK2 inhibitors can affect the atypical kinase Rio1 in a nanomolar range. Kinetic data confirmed the mode of action of benzimidazoles as typical ATP-competitive inhibitors. In contrast to toyocamycin-the first discovered small-molecule inhibitor of Rio1-the most potent representative of benzimidazoles TIBI (IC50 = 0.09 µM, K i = 0.05 µM) does not influence the oligomeric state of the Rio1 kinase. Docking studies revealed that TIBI can occupy the ATP-binding site of Rio1 in a manner similar to toyocamycin, and enhances the thermostability of the enzyme.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP53850-B	5,6-Dichlorobenzimidazole 1-β-D-ribofuranoside		53-85-0	Price

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