N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide

DescriptionH-89 (127243-85-0) is a commonly used inhibitor of protein kinase A (PKA IC50= 140 nM). Inhibits a variety of other kinases including S6K1 (IC50= 80 nM), MSK1 (120 nM), ROCK II (270 nM), PKBα (2.6 μM), PKD, PRK2, RSK1 and 2, SGK, AMPK, CHK1 and MAPKAP-K1b (2.8 μM).1,2

UsesSelective inhibitor of Protein Kinase A (cyclic AMP-dependeant Protein Kinase) with an inhibitory constant of 0.0048 uM.

General DescriptionA cell-permeable, selective, reversible, ATP-competitive and potent inhibitor of protein kinase A (Ki = 48 nM). Inhibits other kinases at several fold higher concentrations: myosin light chain kinase (Ki = 28.3 μM), Ca2+/calmodulin-dependent protein kinase II (Ki = 29.7 μM), protein kinase C (Ki = 31.7 μM), casein kinase I (Ki = 38.3 μM), and Rho Kinase II (IC50 = 270 nM). May be used to discriminate between the effects of PKA and cAMP-regulated guanine-nucleotide-exchange factors (GEFs), such as GEFI or Epac (exchange protein directly activated by cAMP) and GEFII. Reported to induce neurite formation in NG 108-15 cells (~1 mM) by blocking the action of Rho kinase II.