CAS NO: | 127243-85-0 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | 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& Target | IC50: 48 nM (protein kinase A) |
体外研究 (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[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]. |
体内研究 (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[3]. |
分子量 | 446.36 |
Formula | C20H20BrN3O2S |
CAS 号 | 127243-85-0 |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |