Description
H-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
Chemical Properties
White Solid
Uses
Selective inhibitor of Protein Kinase A (cyclic AMP-dependeant Protein Kinase) with an inhibitory constant of
0.0048 uM
Uses
Selective inhibitor of Protein Kinase A (cyclic AMP-dependeant Protein Kinase) with an inhibitory constant of 0.0048 uM.
Definition
ChEBI: A member of the class of isoquinolines that is the sulfonamide obtained by formal condensation of the sulfo group of isoquinoline-5-sulfonic acid with the primary amino group of N1-[3-(4-bromophenyl)prop-2-en-1-yl]et
ane-1,2-diamine.
General Description
A 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.
Biological Activity
Protein kinase A inhibitor that also inhibits several other kinases (IC 50 values are 80, 120, 135, 270, 2600 and 2800 nM for S6K1, MSK1, PKA, ROCKII, PKB α and MAPKAP-K1b).
Biochem/physiol Actions
Target Ki: 48 nM for protein kinase A
References
1) Lochner and Moolman (2006),?The many faces of H89: a review; Cardiovasc. Drugs,?24?261
2) Bain?et al. (2007),?The selectivity of protein kinase inhibitors: a further update; Biochem.J.?408(Pt3)?297
