C-1 是一种有效的蛋白激酶抑制剂,IC50 为 4 μM, 8 μM, 12 μM 和 240 μM 用于 cGMP 依赖性蛋白激酶 (PKG)、cAMP 依赖性蛋白激酶 (PKA) ,分别为蛋白激酶 C (PKC) 和 MLC 激酶。 C-1 也用作 ROCK 抑制剂。
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HA-100 is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase with IC50s of 4, 8, 12 and 240 μM, respectively[1].
HA-100 inhibits MLC-kinase and PKC competitively with respect to ATP, and the Ki values are 61 and 6.5 μM, respectively[1].
参考文献:
[1]. Hagiwara M, et al. Selective modulation of calcium-dependent myosin phosphorylation by novel protein kinase inhibitors, isoquinolinesulfonamide derivatives. Mol Pharmacol. 1987 Jul;32(1):7-12.
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