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Submit ReviewKN-62
说明： Non-competitive P2X7 antagonist
化学名： 4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl] phenyl isoquinolinesulfonic acid ester
纯度： ≥98% (HPLC)
生物活性 for KN-62
KN-62 is a selective, cell-permeable inhibitor of CaM kinase II (IC50 = 0.9 μM). Binds directly to the calmodulin binding site of the enzyme. Potent non-competitive antagonist at the P2X7 receptor (IC50 = 15 nM).
技术数据 for KN-62
| 分子量 | 721.84 |
| 公式 | C38H35N5O6S2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 127191-97-3 |
| PubChem ID | 5312126 |
| InChI Key | RJVLFQBBRSMWHX-DHUJRADRSA-N |
| Smiles | O=S(C1=CC=CC2=C1C=CN=C2)(N(C)[C@H](C(N4CCN(C7=CC=CC=C7)CC4)=O)CC3=CC=C(OS(C5=CC=CC6=C5C=CN=C6)(=O)=O)C=C3)=O |
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 KN-62
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 72.18 | 100 |
制备储备液 for KN-62
以下数据基于产品分子量 721.84。 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 | 1.39 mL | 6.93 mL | 13.85 mL |
| 5 mM | 0.28 mL | 1.39 mL | 2.77 mL |
| 10 mM | 0.14 mL | 0.69 mL | 1.39 mL |
| 50 mM | 0.03 mL | 0.14 mL | 0.28 mL |
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产品说明书 for KN-62
参考文献 for KN-62
参考文献是支持产品生物活性的出版物。
Chessell et al (1998) Effects of antagonists at the human recombinant P2X7 receptor. Br.J.Pharmacol. 124 1314 PMID: 9720806
Hidaka and Yokokura (1996) Molecular and cellular pharmacology of a calcium/calmodulin-dependent protein kinase II (CaM kinase II) inhibitor, KN-62, and proposal of CaM kinase phosphorylation cascades. Adv.Pharmacol. 36 193 PMID: 8783561
Tokumitsu et al (1990) KN-62, 1-[N-O-bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazine, a specific inhibitor of Ca2+/calmodulin-dependent protein kinase II. J.Biol.Chem. 265 4315 PMID: 2155222
If you know of a relevant reference for KN-62, please let us know.
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关键词: KN-62, KN-62 supplier, CaM, kinase, II, inhibitors, inhibits, Non-competitive, P2X7, antagonists, Calmodulin-Activated, calmodulin-dependent, Protein, Kinase, Kinases, Ca2+, Binding, modulators, Calcium, Signaling, Signalling, Receptors, Purinergic, purinoceptors, P2X, 1277, Tocris Bioscience
28 篇 KN-62 的引用文献
引用文献是使用了 Tocris 产品的出版物。 KN-62 的部分引用包括：
Galván et al (2015) Synapse-specific compartmentalization of signaling cascades for LTP induction in CA3 interneurons. Neuroscience 290 332 PMID: 25637803
Braganhol et al (2015) Nucleotide receptors control IL-8/CXCL8 and MCP-1/CCL2 secretions as well as proliferation in human glioma cells. Biochim Biophys Acta 1852 120 PMID: 25445541
Livingstone et al (2019) Secreted Amyloid Precursor Protein-Alpha Promotes Arc Protein Synthesis in Hippocampal Neurons. Front Mol Neurosci 12 198 PMID: 31474829
Sahu et al (2019) Peptide/Receptor Co-evolution Explains the Lipolytic Function of the Neuropeptide TLQP-21. Cell Rep 28 2567 PMID: 31484069
Cui et al (2016) Endocannabinoid dynamics gate spike-timing dependent depression and potentiation. Elife 5 e13185 PMID: 26920222
Qu et al (2016) Neurophysiological mechanisms of bradykinin-evoked mucosal chloride secretion in guinea pig small intestine. World J Gastrointest Pathophysiol 7 150 PMID: 26909238
Finsterwald et al (2013) Role of salt-inducible kinase 1 in the activation of MEF2-dependent transcription by BDNF. PLoS One 8 e54545 PMID: 23349925
Bodhinathan et al (2010) Intracellular redox state alters NMDA receptor response during aging through Ca2+/calmodulin-dependent protein kinase II. J Neurosci 30 1914 PMID: 20130200
Liu and Zhuo (2014) Loss of long-term depression in the insular cortex after tail amputation in adult mice. Mol Pain 10 1 PMID: 24398034
Guo and Feng (2012) OX2R activation induces PKC-mediated ERK and CREB phosphorylation. Exp Cell Res 318 2004 PMID: 22652455
Trabanelli et al (2012) Extracellular ATP exerts opposite effects on activated and regulatory CD4+ T cells via purinergic P2 receptor activation. J Immunol 189 1303 PMID: 22753942
Person and Raman (2010) Deactivation of L-type Ca current by inhibition controls LTP at excitatory synapses in the cerebellar nuclei. Neuron 66 550 PMID: 20510859
Kobayashi et al (2010) Human eosinophils recognize endogenous danger signal crystalline uric acid and produce proinflammatory cytokines mediated by autocrine ATP. J Immunol 184 6350 PMID: 20483787
Mauger et al (2016) Targeted Intron Retention and Excision for Rapid Gene Regulation in Response to Neuronal Activity. Neuron 92 1266 PMID: 28009274
Ledderose et al (2016) Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense. J Infect Dis 213 456 PMID: 26150546
Draganov et al (2015) Modulation of P2X4/P2X7/Pannexin-1 sensitivity to extracellular ATP via iverm. induces a non-apoptotic and inflammatory form of cancer cell death. J Cell Sci 5 16222 PMID: 26552848
Giannuzzo et al (2015) The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells. J Chem Biol 14 203 PMID: 26607222
Oh et al (2015) Heterosynaptic structural plasticity on local dendritic segments of hippocampal CA1 neurons. Neuron 10 162 PMID: 25558061
Araki et al (2015) Rapid dispersion of SynGAP from synaptic spines triggers AMPA receptor insertion and spine enlargement during LTP. PLoS One 85 173 PMID: 25569349
Merino et al (2015) Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with isoprote. Sci Rep 10 e0132884 PMID: 26222156
Heo et al (2015) Biophysical Regulation of Chromatin Architecture Instills a Mechanical Memory in Mesenchymal Stem Cells. Sci Rep 5 16895 PMID: 26592929
Mockett et al (2011) Calcium/calmodulin-dependent protein kinase II mediates group I metabotropic glutamate receptor-dependent protein synthesis and long-term depression in rat hippocampus. J Neurosci 31 7380 PMID: 21593322
George et al (2011) Calcium-dependent phosphorylation regulates neuronal stability and plasticity in a highly precise pacemaker nucleus. J Neurophysiol 106 319 PMID: 21525377
Díaz-Hernández et al (2008) Inhibition of the ATP-gated P2X7 receptor promotes axonal growth and branching in cultured hippocampal neurons. Mol Cancer 121 3717 PMID: 18987356
Ishii and Sugimura (2015) Identification of a new pharmacological activity of the phenylpiperazine derivative naftopidil: tubulin-binding drug. Cell Rep 8 42618 PMID: 25584077
Donnelly-Roberts et al (2009) Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors. Br J Pharmacol 157 1203 PMID: 19558545
Hu et al (2006) Potentiation of TRPV3 channel function by unsaturated fatty acids. J Cell Physiol 208 201 PMID: 16557504
Coba et al (2008) Kinase networks integrate profiles of N-MthD.-aspartate receptor-mediated gene expression in hippocampus. J Biol Chem 283 34101 PMID: 18815127
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KN-62 的评论
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KN62 treatment.
By
Xiaoyu Zhang on 02/07/2024
分析类型： In Vitro
种属： Mouse
细胞系/组织： neuron cells
Mouse neuron culture treated with 10nM KN62. MAP staining showed after treatment.
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