Hagiwara M, Inagaki M, Takahashi J, Yoshida T, Hidaka H
Department of Pharmacology, Nagoya University School of Medicine, Japan.
Pharmacology. 1988;36(6):365-70. doi: 10.1159/000138324.
The isoquinolinesulfonamide compound 1-(5-isoquinolinyl-sulfonyl)-2-methylpiperazine (H-7) has been widely used as a protein kinase C inhibitor. Although H-7 and its derivatives are useful for the demonstration of the biological function of protein kinase C or cyclic nucleotide-dependent protein kinases, these compounds are not available for a histological approach to protein kinase C. In the present study, we introduce 1-(1-hydroxy-5-isoquinolinylsulfonyl)piperazine (hydroxy H-7) as a useful tool in tissue experiments. The property of the compound as a protein kinase C inhibitor was similar to that of H-7. Hydroxy H-7 inhibited the enzyme in a competitive manner with ATP, the Ki value was 23 microM, and exhibited a fluorescence property with a maximum emission wavelength of 444 nm excited at 350 nm. Fluoromicroscopical investigations revealed that hydroxy H-7 penetrated the cell membrane and was distributed mainly in the cytoplasm.
异喹啉磺酰胺化合物1-(5-异喹啉基磺酰基)-2-甲基哌嗪(H-7)已被广泛用作蛋白激酶C抑制剂。尽管H-7及其衍生物对于证明蛋白激酶C或环核苷酸依赖性蛋白激酶的生物学功能很有用，但这些化合物不适用于对蛋白激酶C进行组织学研究。在本研究中，我们引入1-(1-羟基-5-异喹啉基磺酰基)哌嗪(羟基H-7)作为组织实验中的一种有用工具。该化合物作为蛋白激酶C抑制剂的特性与H-7相似。羟基H-7以与ATP竞争性的方式抑制该酶，Ki值为23 microM，并表现出荧光特性，在350 nm激发下最大发射波长为444 nm。荧光显微镜研究表明，羟基H-7穿透细胞膜，主要分布在细胞质中。
