AP-C5 is a potent and selective inhibitor of the guanosine 3′,5′-cyclicmonophosphate (cGMP)-dependent protein kinase II (cGKII)that selectively blocks cGKII dependent phosphorylation of the vasodilator-stimulated phosphoprotein (VASP) in intestinal organoids. AP-C5 mitigates secretory response provoked by the GCC-activating Escherichia coli heat-stable toxin (STa) in mouse small intestinal tissue.
potent and selective inhibitor of the guanosine 3′,5′-cyclicmonophosphate (cGMP)-dependent protein kinase II (cGKII)
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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The Journal of biological chemistry, 293(21), 8173-8181 (2018-04-15)
The guanosine 3',5'-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) serine/threonine kinase relays signaling through guanylyl cyclase C (GCC) to control intestinal fluid homeostasis. Here, we report the discovery of small-molecule inhibitors of cGKII. These inhibitors were imidazole-aminopyrimidines, which blocked recombinant
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