Chemical Name: 4-[4-(1H-Imidazol-1-yl)phenyl]-N-2-propyn-1-yl-2-pyrimidinamine
Biological ActivityPotent 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.
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Selective inhibition of intestinal guanosine 3',5'-cyclic monophosphate signaling by small-molecule protein kinase inhibitors.
Bijvelds et al.
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We developed a model system to form purified alternative pathway (AP) C5 convertases on C3b-coated beads and quantify C5 conversion via functional analysis of released C5a.