Name: H 89 2HCl
Price: 204.00 USD

- Overview
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    Background
    
    H 89 2HCl is a potent PKA inhibitor. In a cell-free assay, the Ki of H 89 is 48 nM, 10-fold selective for PKA than PKG and 500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II [1].
    In vitro:In PC12D cells, pretreatment with H-89 dose-dependently inhibited the forskolin-induced protein phosphorylation, with no influence in intracellular cyclic AMP levels. In PC12D cells, H-89 significantly inhibited the forskolin-induced neurite outgrowth. In PC12D cells, pretreatment with H-89 (30 μM) strikingly inhibited cAMP-dependent histone IIb phosphorylation activity in cell lysates while showed no effects on other protein phosphorylation activity such as cGMP-dependent histone IIb phosphorylation activity [1]. H 89 was a potent and selective PKA inhibitor with Ki of 48 nM in a cell-free assay [2]. H89 also inhibited S6K1, MSK1, PKA, ROCKII, PKBα and MAPKAP-K1b kinases with IC50 of 80, 120, 135, 270, 2600 and 2800 nM, respectively [2]. In the hypotonic medium, 50 μM H89, a concentration commonly used to inhibit PKA, prevented the redistribution response. In normal medium, H89 (50 Μm) induced the redistribution of ERGIC 53 to the ER by 20 min [3].
    
    [1]. 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.
    [2]. Lochner A, Moolman J A. The many faces of H89: a review[J]. Cardiovascular drug reviews, 2006, 24(3‐4): 261-274.
    [3]. 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.
- Properties
  - Alternative Name
    
    (E)-N-(2-((3-(4-bromophenyl)allyl)amino)ethyl)isoquinoline-5-sulfonamide dihydrochloride
    
    CAS Number
    
    130964-39-5
    
    Molecular Formula
    
    C20H20BrN3O2S·2HCl
    
    Molecular Weight
    
    519.28
    
    Appearance
    
    A solid
    
    Purity
    
    99.51%
    
    Solubility
    
    ≥51.9 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 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