H-89

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H-89

CAS No. : 127243-85-0

MCE 国际站：H-89

产品活性：H-89 是一种有效、选择性的 cAMP 依赖性 protein kinase A 抑制剂，IC₅₀ 值为 48 nM，对 PKG，PKC，Casein Kinase 和其他激酶的抑制作用很弱。

研究领域：Stem Cell/Wnt  |  Autophagy

作用靶点：PKA  |  Autophagy

In Vitro: 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. 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.

In Vivo: 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.

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