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 (HA-1077; AT877)是一种非特异性RhoA/ROCK抑制剂，同时抑制蛋白激酶，对ROCK1的Ki为0.33 μM，对ROCK2、PKA、PKC和PKG的IC50值分别为0.158 μM、4.58 μM、12.30 μM和1.650 μM。Fasudil盐酸盐还是一种强效的Ca2+通道拮抗剂和血管扩张剂。

H-89 2HCl是一种高效且选择性的蛋白激酶A（PKA）抑制剂，IC50为48 nM，对PKG、PKC和酪蛋白激酶的抑制作用较弱。

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).

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.