H 89 dihydrochloride
Chemical Name: N-[2-[[3-(4-Bromophenyl)-2-propenyl]amino]ethyl]-5-isoquinolinesulfonamide dihydrochloride
Biological ActivityProtein 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. Also available as part of the PKA TocrisetTM.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Biphasic modulation of nociceptive processing by the cyclic AMP-protein kinase A signalling pathway in sheep spinal cord.
Dolan and Nolan
The many faces of H89: a review.
Lochner and Moolman
Cardiovasc.Drug Rev., 2006;24:261
Amyloid β-peptide inhibition of the PKA/CREB pathway and long-term potentiation: reversibility by drugs that enhance cAMP signaling.
Vitolo et al.
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.
Zhang et al.
Citations for H 89 dihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for H 89 dihydrochloride include:
46 Citations: Showing 1 - 10
Opposing Actions of Adrenocorticotropic Hormone and Glucocorticoids on UCP1-Mediated Respiration in Brown Adipocytes.
Authors: Schnabl Et al.
Front Physiol 2019;9:1931
GPCR signaling inhibits mTORC1 via PKA phosphorylation of Raptor.
Authors: Jewell Et al.
NMDAR-Activated PP1 Dephosphorylates GluN2B to Modulate NMDAR Synaptic Content.
Authors: Chiu Et al.
Cell Rep 2019;28:332
Onion peel extract and its constituent, quercetin inhibits human Slo3 in a pH and calcium dependent manner.
Authors: Wijerathne Et al.
Korean J Physiol Pharmacol 2019;23:381
Aging Increases Hippocampal DUSP2 by a Membrane Cholesterol Loss-Mediated RTK/p38MAPK Activation Mechanism.
Authors: Martín-Segura Et al.
Front Neurol 2019;10:675
MicroRNA-130a Contributes to Type-2 Classical DC-activation in Sj�gren's Syndrome by Targeting Mitogen- and Stress-Activated Protein Kinase-1.
Authors: Lopes Et al.
Front Immunol 2019;10:1335
Rab46 integrates Ca2+ and histamine signaling to regulate selective cargo release from Weibel-Palade bodies.
Authors: Miteva Et al.
J Cell Biol 2019;
Inhibition of cytokine-mediated JNK signalling by purinergic P2Y11 receptors, a novel protective mechanism in endothelial cells.
Cell Signal 2018;51:59
Protein kinase A activation inhibits DUX4 gene expression in myotubes from patients with facioscapulohumeral muscular dystrophy.
Authors: Cruz Et al.
J Biol Chem 2018;293:11837
Autocrine-paracrine prostaglandin E2 signaling restricts TLR4 internalization and TRIF signaling.
Authors: Perkins Et al.
Phosphatases control PKA-dependent functional microdomains at the outer mitochondrial membrane.
Authors: Burdyga Et al.
Proc Natl Acad Sci U S A. 2018;115(28):E6497
Stress hormones promote EGFR inhibitor resistance in NSCLC: Implications for combinations with β-blockers.
Sci Transl Med 2017;9(415):eaao4307
DA D2 receptor-mediated neuroprotection in a G2019S Lrrk2 genetic model of Parkinson�s disease.
Authors: Tozzi Et al.
Cell Death Dis 2017;9(2):204
Differentiation of human umbilical cord Wharton's jelly-derived mesenchymal stem cells into endometrial cells.
Authors: Shi Et al.
Stem Cell Res Ther 2017;8:246
TDAG8 involved in initiating inflammatory hyperalgesia and establishing hyperalgesic priming in mice.
Sci Rep 2017;7:41415
Multiplexing PKA and ERK12 kinases FRET biosensors in living cells using single excitation wavelength dual colour FLIM.
Authors: Demeautis Et al.
Sci Rep 2017;7:41026
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 2017;7:39905
Prostaglandin E2-mediated adenosinergic effects on CD14+ cells: Self-amplifying immunosuppression in cancer.
Authors: Al-Taei Et al.
Extra-mitochondrial prosurvival BCL-2 proteins regulate gene transcription by inhibiting the SUFU tumour suppressor.
Authors: Wu Et al.
Nat Cell Biol 2017;19:1226
Anthrax edema toxin disrupts distinct steps in Rab11-dependent junctional transport.
Authors: Guichard Et al.
PLoS Pathog 2017;13:e1006603
Identification of small molecules that improve ATP synthesis defects conferred by Leber's hereditary optic neuropathy mutations.
Authors: Datta Et al.
Phosphorylation state-dependent modulation of spinal glycine receptors alleviates inflammatory pain.
Authors: Acuña Et al.
J Clin Invest 2016;126:2547
DA 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
Protection against β-amyloid-induced synaptic and memory impairments via altering β-amyloid assembly by bis(heptyl)-cognitin.
Authors: Chang Et al.
Sci Rep 2015;5:10256
Retroactive modulation of spike timing-dependent plasticity by DA.
Authors: Brzosko Et al.
Different patterns of electrical activity lead to long-term potentiation by activating different intracellular pathways.
Authors: Zhu Et al.
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
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
Regulation of AMPA receptor phosphorylation by the neuropeptide PACAP38.
Authors: Toda and Huganir
J Neurosci 2015;112:6712
Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with isoprote.
Authors: Merino Et al.
PLoS One 2015;10:e0132884
DA Promotes Motor Cortex Plasticity and Motor Skill Learning via PLC Activation.
Authors: Rioult-Pedotti Et al.
Cell Death Dis 2015;10:e0124986
Prostaglandin E2 promotes features of replicative senescence in chronically activated human CD8+ T cells.
Authors: Chou Et al.
PLoS One 2014;9:e99432
GABAB receptor phosphorylation regulates KCTD12-induced K+ current desensitization.
Authors: Adelfinger Et al.
Biochem Pharmacol 2014;91:369
Separate cyclic AMP sensors for neuritogenesis, growth arrest, and survival of neuroendocrine cells.
Authors: Emery Et al.
J Biol Chem 2014;289:10126
δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes.
Authors: Liang Et al.
Biochim Biophys Acta 2014;171:5417
Pain modulators regulate the dynamics of PKA-RII phosphorylation in subgroups of sensory neurons.
Authors: Isensee Et al.
J Cell Sci 2014;127:216
Acute SimV. inhibits K ATP channels of porcine coronary artery myocytes.
Authors: Seto Et al.
PLoS One 2013;8:e66404
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
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
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
Melanocortin 4 receptors reciprocally regulate sympathetic and parasympathetic preganglionic neurons.
Authors: Sohn Et al.
Mol Pharmacol 2013;152:612
The expression and relaxant effect of bitter taste receptors in human bronchi.
Authors: Grassin-Delyle Et al.
Respir Res 2013;14:134
The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
Authors: Lee Et al.
β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.
Authors: Meitzen Et al.
J Neurochem 2011;116:984
Competitive regulation of synaptic Ca2+ influx by D2 DA and A2A adenosine receptors.
Authors: Higley and Sabatini
Nat Neurosci 2010;13:958
IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4.
Authors: Chung Et al.
J Endocrinol 2007;194:77
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