KT5823

Potent, selective inhibitor of PKG

Pack Size

Biological Description Potent, selective, reversible inhibitor of Protein Kinase G (PKG) (K_i = 234 nM). Derivative of K252, selective over PKA and PKC (K_i values are >10 μM and 4 μM respectively). Prevents increased phosphorylation of regulators of G-protein-signalling in vivo.
Useful References
KT5823 inhibits cGMP-dependent protein kinase activity in vitro but not in intact human platelets and rat mesangial cells. abstract Pedram (2000) Natriuretic peptides inhibit G protein activation. Mediation through cross-talk between cyclic GMP-dependent protein kinase and regulators of G protein-signaling proteins. J Biol Chem. 10:7365-72. abstract Guanylyl cyclase inhibitors NS2028 and ODQ and protein kinase G (PKG) inhibitor KT5823 trigger apoptotic DNA fragmentation in immortalized uterine epithelial cells: anti-apoptotic effects of basal cGMP/PKG. abstract
Chemical Information (9S,10R,12R)-2,3,9,10,11,12-Hexahydro-10-methoxy-2,9-dimethyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, methyl ester
	Desiccate at -20°C MW 495.53 Soluble in DMSO to 50 mM and in ethanol to 2.5 mM C₂₉H₂₅N₃O₅ 126643-37-6