The many faces of H89: a review

Cardiovasc Drug Rev. Fall-Winter 2006;24(3-4):261-74. doi: 10.1111/j.1527-3466.2006.00261.x.

Abstract

H89 is marketed as a selective and potent inhibitor of protein kinase A (PKA). Since its discovery, it has been used extensively for evaluation of the role of PKA in the heart, osteoblasts, hepatocytes, smooth muscle cells, neuronal tissue, epithelial cells, etc. Despite the frequent use of H89, its mode of specific inhibition of PKA is still not completely understood. It has also been shown that H89 inhibits at least 8 other kinases, while having a relatively large number of PKA-independent effects which may seriously compromise interpretation of data. Thus, while recognizing its kinase inhibiting properties, it is advised that H89 should not be used as the single source of evidence of PKA involvement. H-89 should be used in conjunction with other PKA inhibitors, such as Rp-cAMPS or PKA analogs.

Publication types

  • Review

MeSH terms

  • Animals
  • Cyclic AMP-Dependent Protein Kinases / antagonists & inhibitors*
  • Cyclic AMP-Dependent Protein Kinases / chemistry
  • Isoquinolines / pharmacology*
  • Protein Kinase Inhibitors / pharmacology*
  • Sulfonamides / pharmacology*

Substances

  • Isoquinolines
  • Protein Kinase Inhibitors
  • Sulfonamides
  • Cyclic AMP-Dependent Protein Kinases
  • N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide