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抑制剂/激活剂

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凋亡与自噬

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H-89 dihydrochloride

H-89 dihydrochloride

H-89 dihydrochloride 是一种有效、选择性的 cAMP 依赖性蛋白激酶A (PKA) 抑制剂，IC50 值为 48 nM。也可轻微抑制 PKG，PKC，酪蛋白激酶活性。

货号：
TK0502
规格：

5mg

10mg

50mg

100mg
价格：
￥0.00

产品参数

CAS No.	130964-39-5
生物活性	H-89 dihydrochloride is a potent and selective inhibitor of protein kinase A (PKA) with an IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase.
分子式	C20H24BrCl2N3O3S
分子量	519.28
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 100 mg/mL (192.57 mM; Need ultrasonic) H2O : 5 mg/mL (9.63 mM; ultrasonic and warming and heat to 80°C)
体内研究	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.
体外研究	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 Ca uptake by the SR and affectes the Ca-sensitivity of the contractile apparatus in rat skinned fibres.
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纯度及产品资料	98%

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