H 89 dihydrochloride

Cat. No. 2910

H 89 dihydrochloride C20H20BrN3O2S.2HCl [130964-39-5]

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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.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

Lochner and Moolman (2006) The many faces of H89: a review. Cardiovasc.Drug Rev. 24 261. PMID: 17214602.

Yamada et al (2006) Involvement of cAMP response element-binding protein activation in salivary secretion. Pathobiology 73 1. PMID: 16785762.

Vitolo et al (2002) Amyloid β-peptide inhibition of the PKA/CREB pathway and long-term potentiation: reversibility by drugs that enhance cAMP signaling. Proct.Natl.Acad.Sci.USA 99 13217. PMID: 12244210.

Dolan and Nolan (2001) Biphasic modulation of nociceptive processing by the cyclic AMP-protein kinase A signalling pathway in sheep spinal cord. Neurosci.Lett. 309 157. PMID: 11514065.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for H 89 dihydrochloride include:

Brzosko et al (2015) Retroactive modulation of spike timing-dependent plasticity by dopamine. Elife 4. PMID: 26516682.

Adelfinger et al (2014) GABAB receptor phosphorylation regulates KCTD12-induced K+ current desensitization. Biochem Pharmacol 91 369. PMID: 25065880.

Chou et al (2014) Prostaglandin E2 promotes features of replicative senescence in chronically activated human CD8+ T cells. PLoS One 9 e99432. PMID: 24918932.

Isensee et al (2014) Pain modulators regulate the dynamics of PKA-RII phosphorylation in subgroups of sensory neurons. J Cell Sci 127 216. PMID: 24190886.

Grassin-Delyle et al (2013) The expression and relaxant effect of bitter taste receptors in human bronchi. Respir Res 14 134. PMID: 24266887.

Jahchan et al (2013) A drug repositioning approach identifies tricyclic antidepressants as inhibitors of small cell lung cancer and other neuroendocrine tumors. Cancer Discov 3 1364. PMID: 24078773.

Lee et al (2012) The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP. Nature 492 123. PMID: 23143333.

Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984. PMID: 21143600.

Higley and Sabatini (2010) Competitive regulation of synaptic Ca2+ influx by D2 dopamine and A2A adenosine receptors. Nat Neurosci 13 958. PMID: 20601948.

Chung et al (2007) IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4. J Endocrinol 194 77. PMID: 17592023.

Do you know of a great paper that uses H 89 dihydrochloride from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: H 89 dihydrochloride, supplier, Protein, kinases, A, inhibitors, PKA, H89, dihydrochloride, Tocris Bioscience, Protein Kinase A Inhibitor products

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