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Submit ReviewKN 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.
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 50.1 | 100 温和加热 |
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 |
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.
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
引用文献是使用了 Tocris 产品的出版物。 KN 93 的部分引用包括:
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
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
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
Pedersen et al (2009) Calmodulin kinase II initiates arrhythmogenicity during metabolic acidification in murine hearts. Acta Physiol (Oxf) 197 13 PMID: 19416122
Xu et al (2009) HyperDArgic tone erodes prefrontal long-term potential via a D2 receptor-operated protein phosphatase gate. MBio 29 14086 PMID: 19906957
Galván et al (2015) Synapse-specific compartmentalization of signaling cascades for LTP induction in CA3 interneurons. Neuroscience 290 332 PMID: 25637803
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
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
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
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
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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.