K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases
H Kase, K Iwahashi, S Nakanishi, Y Matsuda… - Biochemical and …, 1987 - Elsevier
H Kase, K Iwahashi, S Nakanishi, Y Matsuda, K Yamada, M Takahashi, C Murakata, A Sato…
Biochemical and biophysical research communications, 1987•ElsevierAbstract K-252 compounds (K-252a and b isolated from Nocardiopsis sp.(1) and their
synthetic derivatives) were found to inhibit cyclic nucleotide-dependent protein kinases and
protein kinase C to various extents. The inhibitions were of the competitive type with respect
to ATP. K-252a was a non-selective inhibitor for these three protein kinases with Ki values
18–25 nM. K-252b showed a comparable potency for protein kinase C (Ki, 20nM), whereas
inhibitory potencies for cyclic nucleotide-dependent protein kinases were reduced. KT5720 …
synthetic derivatives) were found to inhibit cyclic nucleotide-dependent protein kinases and
protein kinase C to various extents. The inhibitions were of the competitive type with respect
to ATP. K-252a was a non-selective inhibitor for these three protein kinases with Ki values
18–25 nM. K-252b showed a comparable potency for protein kinase C (Ki, 20nM), whereas
inhibitory potencies for cyclic nucleotide-dependent protein kinases were reduced. KT5720 …
Abstract
Abstract K-252 compounds (K-252a and b isolated from Nocardiopsis sp.(1) and their synthetic derivatives) were found to inhibit cyclic nucleotide-dependent protein kinases and protein kinase C to various extents. The inhibitions were of the competitive type with respect to ATP. K-252a was a non-selective inhibitor for these three protein kinases with Ki values 18–25 nM. K-252b showed a comparable potency for protein kinase C (Ki, 20nM), whereas inhibitory potencies for cyclic nucleotide-dependent protein kinases were reduced. KT5720 and KT5822 selectively inhibited cAMP-dependent (Ki, 60nM) and cGMP-dependent (Ki, 2.4 nM) protein kinases, respectively.
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