The activity of cGMP-dependent protein kinase (PKG) is controlled by factors that elevate cellular cGMP, like nitric oxide (NO), and by those that reduce cGMP levels, like certain phosphodiesterases. KT 5823 is a potent, selective inhibitor of PKG (in vitro IC50 = 234 nM).1 KT 5823 is cell-permeable and is often used in intact cells to assess the role of PKG in signaling, although there are cases where it poorly inhibits PKG in cells.2 KT 5823 is a weak inhibitor of PKC (Ki = 4 µM) and PKA (Ki >10 µM).1
1
Hidaka, H., and Kobayashi, R. Pharmacology of protein kinase inhibitors. Annu Rev Pharmacol Toxicol32377-397(1992).
2
Burkhardt, M., Glazova, M., Gambaryan, S., et al. KT5823 inhibits cGMP-dependent protein kinase activity in vitro but not in intact human platelets and rat mesangial cells. J Biol Chem275(43)33536-33541(2000).
Hidaka, H., and Kobayashi, R. Pharmacology of protein kinase inhibitors. Annu Rev Pharmacol Toxicol32377-397(1992).
Burkhardt, M., Glazova, M., Gambaryan, S., et al. KT5823 inhibits cGMP-dependent protein kinase activity in vitro but not in intact human platelets and rat mesangial cells. J Biol Chem275(43)33536-33541(2000).
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