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Specificity and mechanism of action of some commonly used protein kinase inhibitors

Specificity and mechanism of action of some commonly used protein kinase inhibitors,10.1042/0264-6021:3510095,Biochemical Journal,Stephen P. DAVIES,He

Specificity and mechanism of action of some commonly used protein kinase inhibitors   (Citations: 1577)
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The specificities of 28 commercially available compounds re- ported to be relatively selective inhibitors of particular serine} threonine-specific protein kinases have been examined against a large panel of protein kinases. The compounds KT 5720, Rottlerin and quercetin were found to inhibit many protein kinases, sometimes much more potently than their presumed targets, and conclusions drawn from their use in cell-based experiments are likely to be erroneous. Ro 318220 and related bisindoylmaleimides, as well as H89, HA1077 and Y 27632, were more selective inhibitors, but still inhibited two or more protein kinases with similar potency. LY 294002 was found to inhibit casein kinase-2 with similar potency to phosphoinositide (phosphatidylinositol) 3-kinase. The compounds with the most impressive selectivity profiles were KN62, PD 98059, U0126, PD
Journal: Biochemical Journal - BIOCHEM J , vol. 351, no. 1, 2000
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