A Selective PKG Inhibitor
KT5823 is a semi-synthetic derivative of K525a. It is a potent, selective inhibitor of cGMP-dependent protein kinase (PKG) (in vitro IC50=234nM). KT5823 interferes at the level of the ATP binding site of the catalytic domain of PKG. The PKG are Ser/Thr protein kinase with broad substrate specificity, and expressed in; brain, smooth muscle cells, platelets, juxtaglomerular kidney cells, and endothelial cells. KT5823 triggered apoptotic DNA fragmentation in immortalized uterine epithelial cells, suggesting a regulatory role for PKG in the apoptotic process in these cells.
Protein Kinase Inhibitors and Activators; PKG Inhibitor.