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Submit ReviewKN 93
说明： CaM kinase II inhibitor; also K+ channel blocker (KV)
化学名： N-[2-[[[3-(4-Chlorophenyl)-2-propenyl]methylamino]methyl]phenyl]-N-(2-hydroxyethyl)-4-methoxybenzenesulphonamide
纯度： ≥98% (HPLC)
生物活性 for KN 93
KN 93 is a potent, cell permeable inhibitor of CaM kinase II (IC50 = 0.37 μM). Also a direct extracellular open channel blocker of voltage-gated potassium channels (IC50 = 307 nM for KV1.5) and abolishes IKr in ventricular myocytes (IC50 = 102.6 nM) independently of CaM kinase II inhibition.
Water soluble form and Negative Control also available.
技术数据 for KN 93
| 分子量 | 501.04 |
| 公式 | C26H29ClN2O4S |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 139298-40-1 |
| PubChem ID | 5312122 |
| InChI Key | LLLQTDSSHZREGW-AATRIKPKSA-N |
| Smiles | O=S(N(CCO)C1=C(CN(C)C/C=C/C3=CC=C(Cl)C=C3)C=CC=C1)(C2=CC=C(OC)C=C2)=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 93
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 50.1 | 100 温和加热 |
制备储备液 for KN 93
以下数据基于产品分子量 501.04。 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 | 2 mL | 9.98 mL | 19.96 mL |
| 5 mM | 0.4 mL | 2 mL | 3.99 mL |
| 10 mM | 0.2 mL | 1 mL | 2 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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产品说明书 for KN 93
参考文献 for KN 93
参考文献是支持产品生物活性的出版物。
Patel et al (1999) Calcium/calmodulin-dependent phosphorylation and activation of human Cdc25-C at the G2/M phase transition in HeLa cells. J.Biol.Chem. 274 7958 PMID: 10075693
Rezazadeh et al (2006) KN-93 (2-[N-(2-Hydroxyethyl)]-N-(4-methoxybenzenesulfonyl)]-amino-N-(4-chlorocinnamyl)-N-methylbenzylamine), a calcium/calmodulin-dependent protein kinase II inhibitor, is a direct extracellular blocker of voltage-gated J.Pharmacol.Exp.Ther. 317 292 PMID: 16368898
Sumi et al (1991) The newly synthesized selective Ca2+/calmodulin dependent protein kinase II inhibitor KN-93 reduces DA content in PC12h cells. Biochem.Biophys.Res.Comm. 181 968 PMID: 1662507
Hegyi et al (2015) KN-93 inhibits IKr in mammalian cardiomyocytes. J.Mol.Cell.Cardiol. 89 173 PMID: 26463508
If you know of a relevant reference for KN 93, please let us know.
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关键词: KN 93, KN 93 supplier, K+, channel, blockers, KV, inhibitors, inhibits, Potassium, Channels, voltage-gated, voltage-dependent, CaM, Kinase, II, kinases, Calmodulin-Activated, calmodulin-dependent, Protein, Ca2+, Binding, modulators, Calcium, Signaling, Signalling, hERG, Human, Ether-A-Go-Go, Gene, KCNQ, K, Voltage-Gated, 1278, Tocris Bioscience
23 篇 KN 93 的引用文献
引用文献是使用了 Tocris 产品的出版物。 KN 93 的部分引用包括：
Abedini et al (2016) WNT5a is required for normal ovarian follicle development and antagonizes g.tropin responsiveness in granulosa cells by suppressing canonical WNT signaling. FASEB J 30 1534 PMID: 26667040
Arguello et al (2014) Involvement of amygdalar protein kinase A, but not calcium/calmodulin-dependent protein kinase II, in the reconsolidation of cocaine-related contextual memories in rats. Psychopharmacology (Berl) 231 55 PMID: 23873418
Guemez-Gamboa et al (2014) Non-cell-autonomous mechanism of activity-dependent neurotransmitter switching. Neuron 82 1004 PMID: 24908484
Gaamouch et al (2012) Interaction between αCaMKII and GluN2B controls ERK-dependent plasticity. J Neurosci 32 10767 PMID: 22855824
Marsden et al (2007) NMDA receptor activation potentiates inhibitory transmission through GABA receptor-associated protein-dependent exocytosis of GABA(A) receptors. J Neurosci 27 14326 PMID: 18160640
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. Apoptosis 5 16222 PMID: 26552848
Bonnefond et al (2015) Calcium signals inhibition sensitizes ovarian carcinoma cells to anti-Bcl-xL strategies through Mcl-1 down-regulation. Oncoscience 20 535 PMID: 25627260
Nygaard et al (2015) Melanoma brain colonization involves the emergence of a brain-adaptive phenotype. Biochem Biophys Res Commun 1 82 PMID: 25593989
Cohen et al (2015) Evolutionary and functional perspectives on signaling from neuronal surface to nucleus. PLoS One 460 88 PMID: 25998737
Kim and Tsien (2008) Synapse-specific adaptations to inactivity in hippocampal circuits achieve homeostatic gain control while dampening network reverberation. Neuron 58 925 PMID: 18579082
Xu et al (2009) HyperDArgic tone erodes prefrontal long-term potential via a D2 receptor-operated protein phosphatase gate. MBio 29 14086 PMID: 19906957
Raka et al (2015) Ca(2+)/calmodulin-dependent protein kinase II interacts with group I metabotropic glutamate and facilitates receptor endocytosis and ERK1/2 signaling: role of β-amyloid. Mol Brain 8 21 PMID: 25885040
Bemben et al (2014) CaMKII phosphorylation of neuroligin-1 regulates excitatory synapses. Nat Neurosci 17 56 PMID: 24336150
Hill and Muldrew (2014) Oestrogen upregulates the sarcoplasmic reticulum Ca(2+) ATPase pump in coronary arteries. Clin Exp Pharmacol Physiol 41 430 PMID: 24684418
Wang et al (2014) SynGAP regulates protein synthesis and homeostatic synaptic plasticity in developing cortical networks. PLoS One 8 e83941 PMID: 24391850
Seto et al (2013) Acute SimV. inhibits K ATP channels of porcine coronary artery myocytes. Biochem Pharmacol 8 e66404 PMID: 23799098
Balasubramanian et al (2013) AMP-activated protein kinase as regulator of P2Y(6) receptor-induced Ins secretion in mouse pancreatic β-cells. J Neurosci 85 991 PMID: 23333427
Weng et al (2017) An Intrinsic Epigenetic Barrier for Functional Axon Regeneration. Neuron 94 337 PMID: 28426967
Glovaci and Chapman (2015) Activation of Phosphatidylinositol-Linked DA Receptors Induces a Facilitation of Glutamate-Mediated Synaptic Transmission in the Lateral Entorhinal Cortex. PLoS One 10 e0131948 PMID: 26133167
Thayer et al (2013) Increased neuronal activity fragments the Golgi complex. Proc Natl Acad Sci U S A 110 1482 PMID: 23297202
Galván et al (2015) Synapse-specific compartmentalization of signaling cascades for LTP induction in CA3 interneurons. Neuroscience 290 332 PMID: 25637803
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
Pedersen et al (2009) Calmodulin kinase II initiates arrhythmogenicity during metabolic acidification in murine hearts. Acta Physiol (Oxf) 197 13 PMID: 19416122
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KN93 ameliorates HOCl-LDL-reduced ICa,L density in cardiomyocytes.
By
Christopher Trummer on 10/22/2018
分析类型： In Vitro
种属： Other
细胞系/组织： Cardiomyocytes
Guinea pig ventricular cardiomyocytes were treated with HOCl-LDL (250 µg/ml, 12-16 h)in the absence or presence of KN93 (5 µM) to follow L-type Ca2+ current (ICa,L) using patch clamp analysis. KN93 ameliorated HOCl-LDL-reduced ICa,L density.
