H-89 is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) withIC₅₀of 48 nM and has weak inhibition on PKG,PKC,Casein Kinase, andotherskinases.

IC50: 48 nM (protein kinase A)

H-89 inhibits protein kinase A, in competitive fashion against ATP. H-89 causes a dose-dependent inhibition of the forskolin-induced protein phosphorylation, with no decrease in intracellular cyclic AMP levels in PC12D cells. H-89 significantly inhibits the forskolin-induced neurite outgrowth from PC12D cells. H-89 (30 μM) inhibits significantly cAMP-dependent histone IIb phosphorylation activity in PC12D cell lysates^[1]. H-89 (1-2 μM) significantly slows the repriming rate in rat skinned fibres, most likely due to it deleteriously affecting the T-system potential. H-89 (10-100 μM) inhibits net Ca²⁺uptake by the SR and affectes the Ca³²-sensitivity of the contractile apparatus in rat skinned fibres^[2].

H-89 (0.2 mg/100g, i.p.) significantly increases seizure latency and threshold in PTZ-treated animals. H-89 (0.05, 0.2 mg/100 g, i.p.) prevents the epileptogenic activity of bucladesine (300 nM) with significant increase of seizure latency and seizure threshold^[3].

446.36

C₂₀H₂₀BrN₃O₂S

127243-85-0

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.