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A Newly Synthesized Selective Casein Kinase I Inhibitor, N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide, and Affinity Purification of Casein Kinase I From Bovine Testis

A Newly Synthesized Selective Casein Kinase I Inhibitor, N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide, and Affinity Purification of Casein Kinase I From Bovine Testis

T Chijiwa, M Hagiwara, H Hidaka

J Biol Chem. 1989 Mar 25;264(9):4924-7.

PMID: 2925675

Abstract:

When screening various isoquinolinesulfonamide compounds which we synthesized, CKI-7, N-(2-amino-ethyl)-5-chloroisoquinoline-8-sulfonamide, was found to have a potent inhibitory action against casein kinase I and a much weaker effect on casein kinase II and other protein kinases. Kinetic analysis indicated that CKI-7 inhibited casein kinase I competitively with respect to ATP and that the Ki values were 8.5 microM for casein kinase I and 70 microM for casein kinase II. An affinity chromatography absorbent was synthesized by coupling CKI-8 (1-(5-chloroisoquinoline-8-sulfonyl], a derivative of CKI-7, to cyanogen bromide-activated Sepharose 4B. Partially purified casein kinase I from bovine testis was subjected to affinity chromatography. Analysis of the purified casein kinase I by polyacrylamide gel electrophoresis in the presence of sodium dodecyl sulfate revealed a single band with molecular weight 37,000. These newly synthesized compounds, CKI-7 and CKI-8, should serve as useful tools for elucidating the biological significance of casein kinase I-mediated reactions.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1177141671	CKI-7 dihydrochloride		1177141-67-1	Price

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