H 89 dihydrochloride

Pricing Availability   Qty
说明: Protein kinase A inhibitor
化学名: N-[2-[[3-(4-Bromophenyl)-2-propenyl]amino]ethyl]-5-isoquinolinesulfonamide dihydrochloride
纯度: ≥98% (HPLC)
说明书
引用文献 (46)
评论 (1)

生物活性 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.

化合物库 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. 了解 Tocris 化合物库的更多信息。

技术数据 for H 89 dihydrochloride

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.

溶解性数据 for H 89 dihydrochloride

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
water 12.98 25
DMSO 51.93 100

制备储备液 for H 89 dihydrochloride

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.

选择批次从而根据批次分子量重新计算:
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

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产品说明书 for H 89 dihydrochloride

分析证书/产品说明书
选择另一批次:

参考文献 for H 89 dihydrochloride

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.

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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

46 篇 H 89 dihydrochloride 的引用文献

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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Product performed ideally over years and would buy again..
By Anonymous on 04/04/2020
分析类型: In Vitro
种属: Rat
细胞系/组织: Sprague-Dawley rats primary neuronal

10 μM H-89 for 30 min

PMID: 31291571 参考文献
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