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Submit ReviewH 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.
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. 了解 Tocris 化合物库的更多信息。
分子量 | 519.28 |
公式 | C20H20BrN3O2S.2HCl |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 12.98 | 25 | |
DMSO | 51.93 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for H 89 dihydrochloride, please let us know.
关键词: H 89 dihydrochloride, H 89 dihydrochloride supplier, Protein, kinases, A, inhibitors, inhibits, PKA, H89, dihydrochloride, Kinase, Stem, Cell, Proliferation, 2910, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 H 89 dihydrochloride 的部分引用包括:
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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10 μM H-89 for 30 min