Home / Protein Kinase A Inhibitors / H 89 dihydrochloride

H 89 dihydrochloride

Catalog #: 2910
46 Citations Datasheet / COA / SDS
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2910/10
2910/50
H 89 dihydrochloride | CAS No. 130964-39-5 | Protein Kinase A Inhibitors
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Description: Protein kinase A inhibitor

Chemical Name: N-[2-[[3-(4-Bromophenyl)-2-propenyl]amino]ethyl]-5-isoquinolinesulfonamide dihydrochloride

Purity: ≥98%

Product Details
Citations (46)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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.

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
    Lee G, Subramanian N, Kim A, Aksentijevich I, Goldbach-Mansky R, Sacks D, Germain R, Kastner D, Chae J
    Nature, 2012;492(7427):123-7.
  2. Specific activation of the G protein-coupled receptor BNGR-A21 by the neuropeptide corazonin from the silkworm, Bombyx mori, dually couples to the G(q) and G(s) signaling cascades.
    Yang, Jingwen, Huang, Haishan, Yang, Huipeng, He, Xiaobai, Jiang, Xue, Shi, Ying, Alatangaole, Damirin, Shi, Liangen, Zhou, Naiming
    J Biol Chem, 2013;288(17):11662-75.
  3. Anthrax edema toxin disrupts distinct steps in Rab11-dependent junctional transport
    A Guichard, P Jain, M Moayeri, R Schwartz, S Chin, L Zhu, B Cruz-Moren, JZ Liu, B Aguilar, A Hollands, SH Leppla, V Nizet, E Bier
    PLoS Pathog., 2017;13(9):e1006603.
  4. Regulation and function of immunosuppressive molecule human leukocyte antigen G5 in human bone tissue.
    Deschaseaux F, Gaillard J, Langonne A, Chauveau C, Naji A, Bouacida A, Rosset P, Heymann D, De Pinieux G, Rouas-Freiss N, Sensebe L
    FASEB J, 2013;27(8):2977-87.
  5. Arachidonic acid triggers [Ca2+]i increases in rat round spermatids by a likely GPR activation, ERK signalling and ER/acidic compartments Ca2+ release
    J Paillamanq, A Sanchez-Tu, EM Carmona, CL Treviño, C Sandoval, F Nualart, N Osses, JG Reyes
    PLoS ONE, 2017;12(2):e0172128.
  6. Protein kinase A activation inhibits DUX4 gene expression in myotubes from patients with facioscapulohumeral muscular dystrophy
    JM Cruz, N Hupper, LS Wilson, JB Concannon, Y Wang, B Oberhauser, K Patora-Kom, Y Zhang, DJ Glass, AU Trendelenb, BA Clarke
    J. Biol. Chem., 2018;0(0):.
  7. Glucagon-like peptide-2 directly regulates hypothalamic neurons expressing neuropeptides linked to appetite control in vivo and in vitro.
    Dalvi PS, Belsham DD
    Endocrinology, 2012;153(5):2385-97.
  8. Telmisartan activates endothelial nitric oxide synthase via Ser1177 phosphorylation in vascular endothelial cells.
    Myojo, Masahiro, Nagata, Daisuke, Fujita, Daishi, Kiyosue, Arihiro, Takahashi, Masao, Satonaka, Hiroshi, Morishita, Yoshiyuk, Akimoto, Tetsu, Nagai, Ryozo, Komuro, Issei, Hirata, Yasunobu
    PLoS ONE, 2014;9(5):e96948.
  9. Sustained signalling by PTH modulates IP3 accumulation and IP3 receptors through cyclic AMP junctions.
    Meena A, Tovey S, Taylor C
    J Cell Sci, 2015;128(2):408-20.
  10. Glucagon-like peptide-1 receptor agonist, exendin-4, regulates feeding-associated neuropeptides in hypothalamic neurons in vivo and in vitro.
    Dalvi PS, Nazarians-Armavil A, Purser MJ, Belsham DD
    Endocrinology, 2012;153(5):2208-22.
  11. Different patterns of electrical activity lead to long-term potentiation by activating different intracellular pathways.
    Zhu G, Liu Y, Wang Y, Bi X, Baudry M
    J Neurosci, 2015;35(2):621-33.
  12. GPR30 regulates glutamate transporter GLT-1 expression in rat primary astrocytes.
    Lee E, Sidoryk-Wegrzynowicz M, Wang N, Webb A, Son D, Lee K, Aschner M
    J Biol Chem, 2012;287(32):26817-28.
  13. Biphasic modulation of nociceptive processing by the cyclic AMP-protein kinase A signalling pathway in sheep spinal cord.
    Dolan and Nolan
    Neurosci.Lett., 2001;309:157
  14. The many faces of H89: a review.
    Lochner and Moolman
    Cardiovasc.Drug Rev., 2006;24:261
  15. Amyloid β-peptide inhibition of the PKA/CREB pathway and long-term potentiation: reversibility by drugs that enhance cAMP signaling.
    Vitolo et al.
    Proct.Natl.Acad.Sci.USA, 2002;99:13217
  16. Lipopolysaccharide suppresses T cells by generating extracellular ATP that impairs their mito-chondrial function via P2Y11 receptors
    K Sueyoshi, C Ledderose, Y Shen, AH Lee, NI Shapiro, WG Junger
    J. Biol. Chem., 2019;0(0):.
  17. 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.
    Hum.Reprod., 2016;31:832

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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

  1. Opposing Actions of Adrenocorticotropic Hormone and Glucocorticoids on UCP1-Mediated Respiration in Brown Adipocytes.
    Authors: Schnabl Et al.
    Front Physiol  2019;9:1931
  2. GPCR signaling inhibits mTORC1 via PKA phosphorylation of Raptor.
    Authors: Jewell Et al.
    Elife  2019;8
  3. NMDAR-Activated PP1 Dephosphorylates GluN2B to Modulate NMDAR Synaptic Content.
    Authors: Chiu Et al.
    Cell Rep  2019;28:332
  4. 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
  5. Aging Increases Hippocampal DUSP2 by a Membrane Cholesterol Loss-Mediated RTK/p38MAPK Activation Mechanism.
    Authors: Martín-Segura Et al.
    Front Neurol  2019;10:675
  6. 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
  7. Rab46 integrates Ca2+ and histamine signaling to regulate selective cargo release from Weibel-Palade bodies.
    Authors: Miteva Et al.
    J Cell Biol  2019;
  8. Inhibition of cytokine-mediated JNK signalling by purinergic P2Y11 receptors, a novel protective mechanism in endothelial cells.
    Authors: Ng
    Cell Signal  2018;51:59
  9. 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
  10. Autocrine-paracrine prostaglandin E2 signaling restricts TLR4 internalization and TRIF signaling.
    Authors: Perkins Et al.
    Nat.Immunol.  2018;19:1309
  11. 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
  12. Stress hormones promote EGFR inhibitor resistance in NSCLC: Implications for combinations with β-blockers.
    Authors: Nilsson
    Sci Transl Med  2017;9(415):eaao4307
  13. 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
  14. 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
  15. TDAG8 involved in initiating inflammatory hyperalgesia and establishing hyperalgesic priming in mice.
    Authors: Dai
    Sci Rep  2017;7:41415
  16. 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
  17. β2-adrenoreceptor Inverse Agonist Down-regulates Muscarine Cholinergic Subtype-3 Receptor and Its Downstream Signal Pathways in Airway Smooth Muscle Cells in vitro.
    Authors: Luo
    Scientific Reports  2017;7:39905
  18. Prostaglandin E2-mediated adenosinergic effects on CD14+ cells: Self-amplifying immunosuppression in cancer.
    Authors: Al-Taei Et al.
    Oncoimmunology  2017;6:e1268308
  19. 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
  20. Anthrax edema toxin disrupts distinct steps in Rab11-dependent junctional transport.
    Authors: Guichard Et al.
    PLoS Pathog  2017;13:e1006603
  21. Identification of small molecules that improve ATP synthesis defects conferred by Leber's hereditary optic neuropathy mutations.
    Authors: Datta Et al.
    Mitochondrion  2016;30:177
  22. Phosphorylation state-dependent modulation of spinal glycine receptors alleviates inflammatory pain.
    Authors: Acuña Et al.
    J Clin Invest  2016;126:2547
  23. 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
  24. 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
  25. Retroactive modulation of spike timing-dependent plasticity by DA.
    Authors: Brzosko Et al.
    Elife  2015;4
  26. Different patterns of electrical activity lead to long-term potentiation by activating different intracellular pathways.
    Authors: Zhu Et al.
    Cell  2015;35:621
  27. 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
  28. 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
  29. Regulation of AMPA receptor phosphorylation by the neuropeptide PACAP38.
    Authors: Toda and Huganir
    J Neurosci  2015;112:6712
  30. Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with isoprote.
    Authors: Merino Et al.
    PLoS One  2015;10:e0132884
  31. DA Promotes Motor Cortex Plasticity and Motor Skill Learning via PLC Activation.
    Authors: Rioult-Pedotti Et al.
    Cell Death Dis  2015;10:e0124986
  32. Prostaglandin E2 promotes features of replicative senescence in chronically activated human CD8+ T cells.
    Authors: Chou Et al.
    PLoS One  2014;9:e99432
  33. GABAB receptor phosphorylation regulates KCTD12-induced K+ current desensitization.
    Authors: Adelfinger Et al.
    Biochem Pharmacol  2014;91:369
  34. Separate cyclic AMP sensors for neuritogenesis, growth arrest, and survival of neuroendocrine cells.
    Authors: Emery Et al.
    J Biol Chem  2014;289:10126
  35. δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes.
    Authors: Liang Et al.
    Biochim Biophys Acta  2014;171:5417
  36. Pain modulators regulate the dynamics of PKA-RII phosphorylation in subgroups of sensory neurons.
    Authors: Isensee Et al.
    J Cell Sci  2014;127:216
  37. Acute SimV. inhibits K ATP channels of porcine coronary artery myocytes.
    Authors: Seto Et al.
    PLoS One  2013;8:e66404
  38. 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
  39. 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
  40. 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
  41. Melanocortin 4 receptors reciprocally regulate sympathetic and parasympathetic preganglionic neurons.
    Authors: Sohn Et al.
    Mol Pharmacol  2013;152:612
  42. The expression and relaxant effect of bitter taste receptors in human bronchi.
    Authors: Grassin-Delyle Et al.
    Respir Res  2013;14:134
  43. The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
    Authors: Lee Et al.
    Nature  2012;492:123
  44. β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.
    Authors: Meitzen Et al.
    J Neurochem  2011;116:984
  45. Competitive regulation of synaptic Ca2+ influx by D2 DA and A2A adenosine receptors.
    Authors: Higley and Sabatini
    Nat Neurosci  2010;13:958
  46. 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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