H 89 2HCl
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
H 89 2HCl是一种有效的PKA抑制剂，在无细胞试验中，Ki为48 nM，对PKA比PKG选择性高10倍，比对PKC、MLCK、钙调蛋白激酶II和酪蛋白激酶I/II选择性高500倍[1]。
体外实验：在PC12D细胞中，H-89预处理以剂量依赖性方式抑制毛喉素诱导的蛋白磷酸化，而细胞内环AMP水平没有降低。H-89也显著抑制毛喉素诱导的PC12D细胞的神经突向外生长。在PC12D细胞中，用H-89（30 μM）预处理显著抑制细胞裂解物中cAMP依赖性组蛋白IIb磷酸化活性，但不影响其它蛋白质的磷酸化活性，例如cGMP依赖性组蛋白IIb的磷酸化活性[1]。H 89是一种选择性和有效的PKA抑制剂，在无细胞试验中Ki为48 nM [2]。H89还抑制一些其他激酶，对S6K1、MSK1、PKA、ROCKII、PKBα和MAPKAP-K1b的IC50分别为80、120、135、270、2600和2800 nM [2]。50 μM 的H89，通常用于抑制PKA的浓度，其在低渗介质中阻止再分布反应。50 μM H89在正常介质中孵育20分钟诱导ERGIC 53再分布到ER [3]。
参考文献：
Chijiwa T, Mishima A, Hagiwara M, 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]. Journal of Biological Chemistry, 1990, 265(9): 5267-5272.
Lochner A, Moolman J A. The many faces of H89: a review[J]. Cardiovascular drug reviews, 2006, 24(3‐4): 261-274.
Lee T H, Linstedt A D. Potential role for protein kinases in regulation of bidirectional endoplasmic reticulum-to-Golgi transport revealed by protein kinase inhibitor H89[J]. Molecular biology of the cell, 2000, 11(8): 2577-2590.
- 1. Xiaodong Kong, Yuting Yang, et al. "GLP‑1 Receptor Agonist Inhibited the Activation of RIPK1 for Alleviation the Neuronal Death and Neuroinflammation in APP/PS1 Mice." International Journal of Peptide Research and Therapeutics. 31 March 2021.
- 2. Liu DT, Hong WS, et al. "Upregulation of adamts9 by gonadotropin in preovulatory follicles of zebrafish." Mol Cell Endocrinol. 2019 Oct 2;499:110608. PMID:31586455
- 3. JianHanaWan, ShuHongac, et al. "The regulation of melanocyte-stimulating hormone on the pigment granule dispersion in the xanthophores and melanophores of the large yellow croaker (Larimichthys crocea)." Aquaculture. Available online 2 April 2019.
- 4. MXinwei Feng, Junfeng Lu, et al. "Mycobacterium smegmatis Induces Neurite Outgrowth and Differentiation in an Autophagy-Independent Manner in PC12 and C17.2 Cells." Front. Cell. Infect. Microbiol., 19 June 2018.
- 5. Matos, Steven Cordeiro, et al. "Peripheral Neuropathy Induces HCN Channel Dysfunction in Pyramidal Neurons of the Medial Prefrontal Cortex." The Journal of Neuroscience 35.38 (2015): 13244-13256. PMID:26400952
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 519.28 |
| Cas No. | 130964-39-5 |
| Formula | C20H20BrN3O2S·2HCl |
| Solubility | ≥51.9 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | (E)-N-(2-((3-(4-bromophenyl)allyl)amino)ethyl)isoquinoline-5-sulfonamide dihydrochloride |
| SDF | Download SDF |
| Canonical SMILES | O=S(C1=CC=CC2=C1C=CN=C2)(NCCNC/C=C/C3=CC=C(Br)C=C3)=O.Cl.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 激酶实验 [1]: | |
|
PKA酶活性测定 |
在终体积为0.2mL，包含50mM Tris-HCl（pH 7.0），10mM乙酸镁，2mM EGTA，1μM cAMP或不含cAMP，3.3-20 μM [γ-32P] ATP（4×105cpm），0.5μg酶，100μg组蛋白H2B和各化合物的反应混合物中测定cAMP依赖性蛋白激酶活性。 |
| 细胞实验 [1]: | |
|
细胞系 |
PC12D细胞 |
|
溶解方法 |
该化合物在DMSO中的溶解度 > 10 mM。若配制更高浓度的溶液，一般步骤如下：请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
|
反应时间 |
30μM、1小时 |
|
应用 |
在PC12D细胞中，H-89（30μM）显著抑制cAMP依赖性组蛋白IIh的磷酸化活性并抑制Forskolin诱导的神经突生长。 |
| 动物实验 [2]: | |
|
动物模型 |
大鼠模型 |
|
剂量 |
20或200 mg/kg，皮下注射，每日两次，共2天 |
|
应用 |
H89引起蛋白质磷酸化的不同修饰，磷酸化中变化最大的是异质核核糖核蛋白（hnRNP），果糖-1,6-二磷酸酶，NSFL1辅因子p47，所有这些都具有与cAMP / PKA潜在的调节关系。 |
|
注意事项 |
请于室内测试所有化合物的溶解度。实际溶解度和理论值可能略有不同，这是由实验系统的误差引起的，属于正常现象。 |
|
References: 1Chijiwa, T., Mishima, A., Hagiwara, M., Sano, M., Hayashi, K., Inoue, T., Naito, K., Toshioka, T. and Hidaka, H. (1990) 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. 265, 5267-5272 2Davis, M. A., Hinerfeld, D., Joseph, S., Hui, Y. H., Huang, N. H., Leszyk, J., Rutherford-Bethard, J. and Tam, S. W. (2006) Proteomic analysis of rat liver phosphoproteins after treatment with protein kinase inhibitor H89 (N-(2-[p-bromocinnamylamino-]ethyl)-5-isoquinolinesulfonamide). J Pharmacol Exp Ther. 318, 589-595 |
|
| Description | H 89 2HCl is a potent inhibitor of PKA with a Ki value of 48 nM. | |||||
| Targets | PKA | S6K1 | ||||
| IC50 | 48 nM(Ki) | 80 nM | ||||
质量控制和MSDS
- 批次:
化学结构
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