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AP C5 选择性抑制鸟苷 3',5'-环单磷酸 (cGMP) 依赖性蛋白激酶 II (cGKII),pIC50 为 7.2,可用于腹泻病的研究。
Potent and selective protein kinase G type II (PKG2) inhibitor (pIC50 = 7.2). Displays >20-fold selectivity for PKG2 over PKG1 and PKA (pIC50 values are 4.6 and 4.8 for PKG1 and PKA, respectively). Blocks 8-pCPT-cGMP-dependent VASP phosphorylation in intestinal organoids. Also attenuates toxin-stimulated anion secretory responses in mouse intestinal tissue.
Bijvelds et al (2018) Selective inhibition of intestinal guanosine 3',5'-cyclic monophosphate signaling by small-molecule protein kinase inhibitors. J.Biol.Chem. 293 8173 PMID:29653944
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