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Submit ReviewH 89 dihydrochloride
Description: Protein kinase A inhibitor
Chemical Name: N-[2-[[3-(4-Bromophenyl)-2-propenyl]amino]ethyl]-5-isoquinolinesulfonamide dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity for H 89 dihydrochloride
H 89 dihydrochloride is a 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. Enhances survival and clonogenicity of dissociated human ESCs through ROCK inhibition.
Compound Libraries for H 89 dihydrochloride
H 89 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.
Technical Data for H 89 dihydrochloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for H 89 dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 12.98 | 25 | |
| DMSO | 51.93 | 100 |
Preparing Stock Solutions for H 89 dihydrochloride
The following data is based on the product molecular weight 519.28. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 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 for H 89 dihydrochloride
References for H 89 dihydrochloride
References are publications that support the biological activity of the product.
Lochner and Moolman (2006) The many faces of H89: a review. Cardiovasc.Drug Rev. 24 261 PMID: 17214602
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
Zhang et al (2016) Protein kinase A inhibitor, H89, enhances survival and clonogenicity of dissociated human embryonic stem cells through Rho-associated coiled-coil containing protein kinase (ROCK) inhibition. Hum.Reprod. 31 832 PMID: 26848187
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Keywords: H 89 dihydrochloride, H 89 dihydrochloride supplier, Protein, kinases, A, inhibitors, inhibits, PKA, H89, dihydrochloride, Kinase, Stem, Cell, Proliferation, 2910, Tocris Bioscience
46 Citations for H 89 dihydrochloride
Citations are publications that use Tocris products. Selected citations for H 89 dihydrochloride include:
Higley and Sabatini (2010) Competitive regulation of synaptic Ca2+ influx by D2 DA and A2A adenosine receptors. Nat Neurosci 13 958 PMID: 20601948
Burdyga et al (2018) Phosphatases control PKA-dependent functional microdomains at the outer mitochondrial membrane. Proc Natl Acad Sci U S A. 115 E6497 PMID: 29941564
Ng (2018) Inhibition of cytokine-mediated JNK signalling by purinergic P2Y11 receptors, a novel protective mechanism in endothelial cells. Cell Signal 51 59 PMID: 30076967
Cruz et al (2018) Protein kinase A activation inhibits DUX4 gene expression in myotubes from patients with facioscapulohumeral muscular dystrophy. J Biol Chem 293 11837 PMID: 29899111
Emery et al (2014) Separate cyclic AMP sensors for neuritogenesis, growth arrest, and survival of neuroendocrine cells. J Biol Chem 289 10126 PMID: 24567337
Perkins et al (2018) Autocrine-paracrine prostaglandin E2 signaling restricts TLR4 internalization and TRIF signaling. Nat.Immunol. 19 1309 PMID: 30397349
Datta et al (2016) Identification of small molecules that improve ATP synthesis defects conferred by Leber's hereditary optic neuropathy mutations. Mitochondrion 30 177 PMID: 27497748
Xing et al (2015) DA 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 isoprote. PLoS One 10 e0132884 PMID: 26222156
Rioult-Pedotti et al (2015) DA Promotes Motor Cortex Plasticity and Motor Skill Learning via PLC Activation. Cell Death Dis 10 e0124986 PMID: 25938462
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
Adelfinger et al (2014) GABAB receptor phosphorylation regulates KCTD12-induced K+ current desensitization. Biochem Pharmacol 91 369 PMID: 25065880
Schnabl et al (2019) Opposing Actions of Adrenocorticotropic Hormone and Glucocorticoids on UCP1-Mediated Respiration in Brown Adipocytes. Front Physiol 9 1931 PMID: 30705635
Guichard et al (2017) Anthrax edema toxin disrupts distinct steps in Rab11-dependent junctional transport. PLoS Pathog 13 e1006603 PMID: 28945820
Demeautis et al (2017) Multiplexing PKA and ERK12 kinases FRET biosensors in living cells using single excitation wavelength dual colour FLIM. Sci Rep 7 41026 PMID: 28106114
Al-Taei et al (2017) Prostaglandin E2-mediated adenosinergic effects on CD14+ cells: Self-amplifying immunosuppression in cancer. Oncoimmunology 6 e1268308 PMID: 28344879
Wu et al (2017) Extra-mitochondrial prosurvival BCL-2 proteins regulate gene transcription by inhibiting the SUFU tumour suppressor. Nat Cell Biol 19 1226 PMID: 28945232
Brzosko et al (2015) Retroactive modulation of spike timing-dependent plasticity by DA. Elife 4 PMID: 26516682
Liang et al (2014) δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes. Biochim Biophys Acta 171 5417 PMID: 25052197
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 SimV. inhibits K ATP channels of porcine coronary artery myocytes. PLoS One 8 e66404 PMID: 23799098
Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984 PMID: 21143600
Nilsson (2017) Stress hormones promote EGFR inhibitor resistance in NSCLC: Implications for combinations with β-blockers. Sci Transl Med 9 eaao4307 PMID: 29118262
Shi et al (2017) Differentiation of human umbilical cord Wharton's jelly-derived mesenchymal stem cells into endometrial cells. Stem Cell Res Ther 8 246 PMID: 29096715
Toda and Huganir (2015) Regulation of AMPA receptor phosphorylation by the neuropeptide PACAP38. J Neurosci 112 6712 PMID: 25964356
Martín-Segura et al (2019) Aging Increases Hippocampal DUSP2 by a Membrane Cholesterol Loss-Mediated RTK/p38MAPK Activation Mechanism. Front Neurol 10 675 PMID: 31293510
Lopes et al (2019) MicroRNA-130a Contributes to Type-2 Classical DC-activation in Sjögren's Syndrome by Targeting Mitogen- and Stress-Activated Protein Kinase-1. Front Immunol 10 1335 PMID: 31281310
Chiu et al (2019) NMDAR-Activated PP1 Dephosphorylates GluN2B to Modulate NMDAR Synaptic Content. Cell Rep 28 332 PMID: 31291571
Tozzi et al (2017) DA D2 receptor-mediated neuroprotection in a G2019S Lrrk2 genetic model of Parkinson’s disease. Cell Death Dis 9 204 PMID: 29434188
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
Chang et al (2015) Protection against β-amyloid-induced synaptic and memory impairments via altering β-amyloid assembly by bis(heptyl)-cognitin. Sci Rep 5 10256 PMID: 26194093
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
Jewell et al (2019) GPCR signaling inhibits mTORC1 via PKA phosphorylation of Raptor. Elife 8 PMID: 31112131
Miteva et al (2019) Rab46 integrates Ca2+ and histamine signaling to regulate selective cargo release from Weibel-Palade bodies. J Cell Biol PMID: 31092558
Wijerathne et al (2019) Onion peel extract and its constituent, quercetin inhibits human Slo3 in a pH and calcium dependent manner. Korean J Physiol Pharmacol 23 381 PMID: 31496875
Acuña et al (2016) Phosphorylation state-dependent modulation of spinal glycine receptors alleviates inflammatory pain. J Clin Invest 126 2547 PMID: 27270175
Lee et al (2012) The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP. Nature 492 123 PMID: 23143333
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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Product performed ideally over years and would buy again..
By
Anonymous on 04/04/2020
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: Sprague-Dawley rats primary neuronal
10 μM H-89 for 30 min
