产品描述
H-89 is a selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A; IC50: 48 nM). H-89 has weak inhibition on PKG, Casein Kinase, PKC, and other kinases.
体外活性
H-89 (30 μM) inhibits significantly cAMP-dependent histone IIb phosphorylation activity in PC12D cell lysates. 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.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.
体内活性
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.H-89 (0.2 mg/100g, i.p.) significantly increases seizure latency and threshold in PTZ-treated animals.
Cas No.
127243-85-0
分子式
C20H20BrN3O2S
分子量
446.36
别名
Protein kinase inhibitor H-89;H-89
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years