Biological descriptionPotent, selective, reversible inhibitor of Protein Kinase G (PKG) (Ki = 234 nM). Derivative of K252, selective over PKA and PKC (Ki values are >10 and 4 μM, respectively). Prevents increased phosphorylation of regulators of G-protein-signalling in vivo.
Chemical name(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
Storage instructionsStore at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Solubility overviewSoluble in DMSO to 50 mM and in ethanol to 2.5 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Chan SL & Fiscus RR 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. Mol Hum Reprod9:775-83 (2003).
Read more (PubMed: 14614039) »
Burkhardt M et al. KT5823 inhibits cGMP-dependent protein kinase activity in vitro but not in intact human platelets and rat mesangial cells. J Biol Chem275:33536-41 (2000).
Read more (PubMed: 10922374) »