Catalog Number: 2910
Chemical Name: N-[2-[[3-(4-Bromophenyl)-2-propenyl]amino]ethyl]-5-isoquinolinesulfonamide dihydrochloride
Biological Activity
Protein kinase A inhibitor that also inhibits several other kinases (IC50 values are 80, 120, 135, 270, 2600 and 2800 nM for S6K1, MSK1, PKA, ROCKII, PKBα and MAPKAP-K1b). Exhibits antinociceptive activity. Also available as part of the PKA TocrisetTM.
Technical Data
  • M.Wt:
    519.28
  • Formula:
    C20H20BrN3O2S.2HCl
  • Solubility:
    Soluble to 25 mM in water and to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    130964-39-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. The many faces of H89: a review.
    Lochner and Moolman
    Cardiovasc.Drug Rev., 2006;24:261
  2. Involvement of cAMP response element-binding protein activation in salivary secretion.
    Yamada et al.
    Pathobiology, 2006;73:1
  3. Amyloid β-peptide inhibition of the PKA/CREB pathway and long-term potentiation: reversibility by drugs that enhance cAMP signaling.
    Vitolo et al.
    Proct.Natl.Acad.Sci.USA, 2002;99:13217
  4. Biphasic modulation of nociceptive processing by the cyclic AMP-protein kinase A signalling pathway in sheep spinal cord.
    Dolan and Nolan
    Neurosci.Lett., 2001;309:157
Citations:

The citations listed below are publications that use Tocris products. Selected citations for H 89 dihydrochloride include:

24 Citations: Showing 1 - 10
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  1. TDAG8 involved in initiating inflammatory hyperalgesia and establishing hyperalgesic priming in mice.
    Authors: Dai
    Sci Rep 2017;7:41415?
  2. β2-adrenoreceptor Inverse Agonist Down-regulates Muscarine Cholinergic Subtype-3 Receptor and Its Downstream Signal Pathways in Airway Smooth Muscle Cells in vitro.
    Authors: Luo
    Scientific Reports 2017;7:39905
  3. Dopamine D1 receptor activation regulates the expression of the estrogen synthesis gene aromatase B in radial glial cells.
    Authors: Xing Et al.
    Br J Pharmacol 2015;9:310
  4. Retroactive modulation of spike timing-dependent plasticity by dopamine.
    Authors: Brzosko Et al.
    Elife 2015;4
  5. Different patterns of electrical activity lead to long-term potentiation by activating different intracellular pathways.
    Authors: Zhu Et al.
    Cell 2015;35:621
  6. Phosphorylation of ezrin on Thr567 is required for the synergistic activation of cell spreading by EPAC1 and protein kinase A in HEK293T cells.
    Authors: Parnell Et al.
    Mol Med Rep 2015;1853:1749
  7. A long-acting β2-adrenergic agonist increases the expression of muscarine cholinergic subtype-3 receptors by activating the β2-adrenoceptor cyclic adenosine monophosphate signaling pathway in airway smooth muscle cells.
    Authors: Liu Et al.
    Proc Natl Acad Sci U S A 2015;11:4121
  8. Regulation of AMPA receptor phosphorylation by the neuropeptide PACAP38.
    Authors: Toda and Huganir
    J Neurosci 2015;112:6712
  9. Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with Isoproterenol.
    Authors: Merino Et al.
    PLoS One 2015;10:e0132884
  10. Dopamine Promotes Motor Cortex Plasticity and Motor Skill Learning via PLC Activation.
    Authors: Rioult-Pedotti Et al.
    Cell Death Dis 2015;10:e0124986
  11. Prostaglandin E2 promotes features of replicative senescence in chronically activated human CD8+ T cells.
    Authors: Chou Et al.
    PLoS One 2014;9:e99432
  12. GABAB receptor phosphorylation regulates KCTD12-induced K+ current desensitization.
    Authors: Adelfinger Et al.
    Biochem Pharmacol 2014;91:369
  13. δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes.
    Authors: Liang Et al.
    Biochim Biophys Acta 2014;171:5417
  14. Pain modulators regulate the dynamics of PKA-RII phosphorylation in subgroups of sensory neurons.
    Authors: Isensee Et al.
    J Cell Sci 2014;127:216
  15. Acute simvastatin inhibits K ATP channels of porcine coronary artery myocytes.
    Authors: Seto Et al.
    PLoS One 2013;8:e66404
  16. PDE3 and PDE4 isozyme-selective inhibitors are both required for synergistic activation of brown adipose tissue.
    Authors: Kraynik Et al.
    PLoS One 2013;83:1155
  17. Neuropeptide Y receptors activation protects rat retinal neural cells against necrotic and apoptotic cell death induced by glutamate.
    Authors: Santos-Carvalho Et al.
    Purinergic Signal 2013;4:e636
  18. A drug repositioning approach identifies tricyclic antidepressants as inhibitors of small cell lung cancer and other neuroendocrine tumors.
    Authors: Jahchan Et al.
    Cancer Discov 2013;3:1364
  19. Melanocortin 4 receptors reciprocally regulate sympathetic and parasympathetic preganglionic neurons.
    Authors: Sohn Et al.
    Mol Pharmacol 2013;152:612
  20. The expression and relaxant effect of bitter taste receptors in human bronchi.
    Authors: Grassin-Delyle Et al.
    Respir Res 2013;14:134
  21. The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
    Authors: Lee Et al.
    Nature 2012;492:123
  22. β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.
    Authors: Meitzen Et al.
    J Neurochem 2011;116:984
  23. Competitive regulation of synaptic Ca2+ influx by D2 dopamine and A2A adenosine receptors.
    Authors: Higley and Sabatini
    Nat Neurosci 2010;13:958
  24. IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4.
    Authors: Chung Et al.
    J Endocrinol 2007;194:77
Expand to show all 24 Citations

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