PKG Drug G1 targets C42 of PKG Iα. PKG drug G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.

Fasudil HCl is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM, respectively.

HA-100 is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase (IC50 values are 4, 8, 12 and 240 μM, respectively).

H 89 2HCl is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM. It also shows weak inhibition on PKG, PKC, CK1, CK2 and others kinases.

HA-100 is an isoquinoline compound with an added piperazinylsulfonyl group that acts as an inhibitor of protein kinases (PKs), including PKA, PKC, and PKG (IC50s = 8, 12, and 4 µM, respectively).

KT 5823 is a selective inhibitor of the cGMP-dependent protein kinase (PKG) (Ki values are 0.23, 4 and > 10 μM for inhibition of PKG, PKC and PKA respectively). KT 5823 inhibits SNP-stimulated PKG activity with an IC50 of 60 nM in dispersed smooth muscle cells and has little effect on PKA activity at concentrations of up to 10 μM.