H 89 dihydrochloride

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Cat.No. 2910 - H 89 dihydrochloride | C20H20BrN3O2S.2HCl | CAS No. 130964-39-5
Description: Protein kinase A inhibitor
Chemical Name: N-[2-[[3-(4-Bromophenyl)-2-propenyl]amino]ethyl]-5-isoquinolinesulfonamide dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (24)
Literature

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.

Compound Libraries

H 89 dihydrochloride is also offered as part of the Tocriscreen Plus, Tocriscreen Kinase Inhibitor Toolbox I and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 519.28
Formula C20H20BrN3O2S.2HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 130964-39-5
PubChem ID 5702541
InChI Key GELOGQJVGPIKAM-WTVBWJGASA-N
Smiles O=S(C2=CC=CC1=CN=CC=C12)(NCCNC/C=C/C3=CC=C(Br)C=C3)=O.Cl.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 51.93 100
water 12.98 25

Preparing Stock Solutions

The following data is based on the product molecular weight 519.28. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.93 mL 9.63 mL 19.26 mL
5 mM 0.39 mL 1.93 mL 3.85 mL
10 mM 0.19 mL 0.96 mL 1.93 mL
50 mM 0.04 mL 0.19 mL 0.39 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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 H 89 dihydrochloride, please let us know.

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Keywords: Protein kinases A inhibitors inhibits PKA H89 dihydrochloride Protein Kinase A

24 Citations for H 89 dihydrochloride

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

Luo (2017) β2-adrenoreceptor Inverse Agonist Down-regulates Muscarine Cholinergic Subtype-3 Receptor and Its Downstream Signal Pathways in Airway Smooth Muscle Cells in vitro. Scientific Reports 7 39905 PMID: 28051147

Dai (2017) TDAG8 involved in initiating inflammatory hyperalgesia and establishing hyperalgesic priming in mice. Sci Rep 7 41415  PMID: 28145512

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

Xing et al (2015) Dopamine D1 receptor activation regulates the expression of the estrogen synthesis gene aromatase B in radial glial cells. Br J Pharmacol 9 310 PMID: 26388722

Parnell et al (2015) Phosphorylation of ezrin on Thr567 is required for the synergistic activation of cell spreading by EPAC1 and protein kinase A in HEK293T cells. Mol Med Rep 1853 1749 PMID: 25913012

Liu et al (2015) 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. Proc Natl Acad Sci U S A 11 4121 PMID: 25672589

Zhu et al (2015) Different patterns of electrical activity lead to long-term potentiation by activating different intracellular pathways. Cell 35 621 PMID: 25589756

Merino et al (2015) Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with Isoproterenol. PLoS One 10 e0132884 PMID: 26222156

Rioult-Pedotti et al (2015) Dopamine Promotes Motor Cortex Plasticity and Motor Skill Learning via PLC Activation. Cell Death Dis 10 e0124986 PMID: 25938462

Toda and Huganir (2015) Regulation of AMPA receptor phosphorylation by the neuropeptide PACAP38. J Neurosci 112 6712 PMID: 25964356

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

Liang et al (2014) δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes. Biochim Biophys Acta 171 5417 PMID: 25052197

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

Santos-Carvalho et al (2013) Neuropeptide Y receptors activation protects rat retinal neural cells against necrotic and apoptotic cell death induced by glutamate. Purinergic Signal 4 e636 PMID: 23681231

Sohn et al (2013) Melanocortin 4 receptors reciprocally regulate sympathetic and parasympathetic preganglionic neurons. Mol Pharmacol 152 612 PMID: 23374353

Kraynik et al (2013) PDE3 and PDE4 isozyme-selective inhibitors are both required for synergistic activation of brown adipose tissue. PLoS One 83 1155 PMID: 23493317

Seto et al (2013) Acute simvastatin inhibits K ATP channels of porcine coronary artery myocytes. PLoS One 8 e66404 PMID: 23799098

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


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