H 89 dihydrochloride

Name: H 89 dihydrochloride
Brand: Tocris Bioscience
SKU: 2910
Rating: 4 (1 reviews)

Catalog # 2910 | Tocris Bioscience a Bio-Techne Brand

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Citations (46)

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Protein kinase A inhibitor

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Key Product Details

Description:	Protein kinase A inhibitor
Chemical Name:	N-[2-[[3-(4-Bromophenyl)-2-propenyl]amino]ethyl]-5-isoquinolinesulfonamide dihydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	519.28

View Full Technical Details for H 89 dihydrochloride

Technical Data
Citations (46) / Reviews (1)

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 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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References for H 89 dihydrochloride

References are publications that support the biological activity of the product.

Zhang 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. 2016 PMID: 26848187
Lochner and Moolman The many faces of H89: a review. Cardiovasc.Drug Rev. 2006 PMID: 17214602
Vitolo 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 2002 PMID: 12244210
Dolan and Nolan Biphasic modulation of nociceptive processing by the cyclic AMP-protein kinase A signalling pathway in sheep spinal cord. Neurosci.Lett. 2001 PMID: 11514065

Citations for H 89 dihydrochloride (46)

Showing 1 - 10 of 46 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for H 89 dihydrochloride include:

Schnabl et al. (2019) Opposing Actions of Adrenocorticotropic Hormone and Glucocorticoids on UCP1-Mediated Respiration in Brown Adipocytes. Front Physiol. 9:1931
PMID: 30705635
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. 2019;
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
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 Sj�gren'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
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
Burdyga et al. (2018) Phosphatases control PKA-dependent functional microdomains at the outer mitochondrial membrane. Proc Natl Acad Sci U S A.. 115(28):E6497
PMID: 29941564
Perkins et al. (2018) Autocrine-paracrine prostaglandin E₂ signaling restricts TLR4 internalization and TRIF signaling. Nat.Immunol.. 19:1309
PMID: 30397349
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
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
Nilsson (2017) Stress hormones promote EGFR inhibitor resistance in NSCLC: Implications for combinations with β-blockers. Sci Transl Med. 9(415):eaao4307
PMID: 29118262
Tozzi et al. (2017) DA D2 receptor-mediated neuroprotection in a G2019S Lrrk2 genetic model of Parkinson�s disease. Cell Death Dis. 9(2):204
PMID: 29434188
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
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
Acuña et al. (2016) Phosphorylation state-dependent modulation of spinal glycine receptors alleviates inflammatory pain. J Clin Invest. 126:2547
PMID: 27270175
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
Brzosko et al. (2015) Retroactive modulation of spike timing-dependent plasticity by DA. Elife. 4
PMID: 26516682
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
Toda and Huganir (2015) Regulation of AMPA receptor phosphorylation by the neuropeptide PACAP38. J Neurosci. 112:6712
PMID: 25964356
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
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
Emery et al. (2014) Separate cyclic AMP sensors for neuritogenesis, growth arrest, and survival of neuroendocrine cells. J Biol Chem. 289:10126
PMID: 24567337
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
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
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
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 DA 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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Product performed ideally over years and would buy again.

Name: Anonymous

Species: Rat

Assay Type: In Vitro

Cell Line/Tissue: Sprague-Dawley rats primary neuronal

10 μM H-89 for 30 min

PMID: 31291571 Reference

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