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H-89

产品编号 T11524 CAS 127243-85-0

别名: Protein kinase inhibitor H-89

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. 在相同实验条件下，摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性，但盐形式 H-89 dihydrochloride 的水溶性和稳定性通常比游离态更好。

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H-89, CAS 127243-85-0

规格	价格/CNY		货期	数量
2 mg	￥ 234		5日内发货
5 mg	￥ 365		5日内发货

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H-89 的其他形式现货产品:

H-89 dihydrochloride

其他形式的 H-89:

H-89 dihydrochloride
现货

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生物活性

化学信息

存储 & 溶解度

参考文献

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.
靶点活性	PKA:48 nM
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.

别名	Protein kinase inhibitor H-89
分子量	446.36
分子式	C20H20BrN3O2S
CAS No.	127243-85-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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浓度

容积

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浓度 (起始)

容积 (起始)

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参考文献

1. Chijiwa T, et al. Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma cells. J Biol Chem. 1990 Mar 25;265(9):5267-72. 2. Blazev R, et al. Effects of the PKA inhibitor H-89 on excitation-contraction coupling in skinned and intact skeletal muscle fibres. J Muscle Res Cell Motil. 2001;22(3):277-86. 3. Hosseini-Zare MS, et al. Effects of pentoxifylline and H-89 on epileptogenic activity of bucladesine in pentylenetetrazol-treated mice. Eur J Pharmacol. 2011 Nov 30;670(2-3):464-70. 4. Ma L, Gong F, Xu J, et al. Uncarboxylated osteocalcin reverses the high glucose‑induced inhibition of the osteogenic differentiation of MC3T3E1 cells via the GPRC6A/cAMP/PKA/AMPK signaling pathway[J]. International Journal of Molecular Medicine. 2021, 47(5): 1-11

文献引用

1. Liu M, Yang Y, Tan B, et al. G αi and G βγ subunits have opposing effects on dexmedetomidine-induced sedation. European Journal of Pharmacology. 2018, 831: 28-37 2. Yu Z, Kong D, Liang Y, et al. Protective effects of VMY-2-95 on corticosterone-induced injuries in mice and cellular models. Acta Pharmaceutica Sinica B. 2021 3. Ma L, Gong F, Xu J, et al. Uncarboxylated osteocalcin reverses the high glucose‑induced inhibition of the osteogenic differentiation of MC3T3E1 cells via the GPRC6A/cAMP/PKA/AMPK signaling pathway. International Journal of Molecular Medicine. 2021 May;47(5):91. doi: 10.3892/ijmm.2021.4924. Epub 2021 Mar 31.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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