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H-89
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
H-89图片
CAS NO:127243-85-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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。
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.