 
        
        
        KN-92 phosphate是 KN-93 的非活性衍生物。KN-93 是一种选择性 Ca2+/钙调蛋白依赖性激酶 II(CaMKII)抑制剂,竞争性地阻断钙调蛋白(CaM)与该激酶的结合(Ki = 370 nM)。
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 HazMat Fee + There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
| Type | HazMat fee for 500 gram (Estimated) | 
| Excepted Quantity | USD 0.00 | 
| Limited Quantity | USD 15-60 | 
| Inaccessible (Haz class 6.1), Domestic | USD 80+ | 
| Inaccessible (Haz class 6.1), International | USD 150+ | 
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ | 
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ | 
 
                                 
                                
                            

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| 产品名称 | CaMKII ↓ ↑ | CaMKIII ↓ ↑ | CaMKKα ↓ ↑ | CaMKKβ ↓ ↑ | PKD ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| KN-62 | + CaMKII, Ki: 0.9 μM | 99% | |||||||||||||||||
| KN-93 | ++ CaMKII, Ki: 0.37 μM | 99% | |||||||||||||||||
| NH125 | +++ eEF-2 kinase, IC50: 60 nM | 99%+ | |||||||||||||||||
| STO-609 | ++ CaM-KKα, Ki: 0.25 μM | ++++ CaM-KKβ, Ki: 47 nM | 98% | ||||||||||||||||
| CID755673 | +++ PKD1, IC50: 180 nM PKD2, IC50: 227 nM | 99%+ | |||||||||||||||||
| CRT0066101 2HCl | ++++ PKD1, IC50: 1 nM PKD2, IC50: 2 nM | 99%+ | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | KN-92 phosphate is an inactive derivative of KN-93, without CaM kinase inhibitory activity[3]. Incubation of 10 micromol/L KN-93 induced the cell growth reduction in a time-dependent manner from 78.27% at 8 h to 11.48% at 48 h. However, KN-92, an inactive derivative of KN-93, did not inhibit cell proliferation effectively[4]. Inhibition of Ca2+/calmodulin kinase (KN-63, KN-92; 5 microM) reduced Cl--conductance in 50% of the cells investigated without affecting [Ca2+]i[5]. The CaMKII inhibitor, KN-93 (N-[2-(N-(4-Chlorocinnamyl)-N-methylaminomethyl)phenyl]-N-[2-hydroxyethyl]-4-methoxybenzenesulfonamide), but not the inactive isomer, KN-92 (2-[N-(4-Methoxybenzenesulfonyl)]amino-N-(4-chlorocinnamyl)-N-methylbenzylamine, phosphate), blocked clozapine's augmenting effect on NMDA-evoked responses in pyramidal cells of the rat mPFC. KN-93 also inhibited the facilitatory effect of clozapine on electrically evoked responses in the pyramidal cells, while KN-92 did not show any effect[6]. | 
| Concentration | Treated Time | Description | References | |
| Rabbit ventricular myocytes | 1 μmol/l | KN-92 had no effect on hypokalemia-induced EADs | Circulation. 2015 Oct 20;132(16):1528-1537. | |
| Rabbit ventricular myocytes | 1 μM | 7.5 ± 1.2 minutes | KN-92, an inactive analog of KN-93, failed to prevent H2O2-induced EADs | Circ Res. 2009 Jan 2;104(1):79-86. | 
| Head kidney macrophages (HKM) | 20 μM | 24 hours | As a structural analogue of KN-93, KN-92 lacks CaM kinase inhibitory activity and is used as an experimental control. | PLoS Pathog. 2014 Apr 24;10(4):e1004018. | 
| HeLa cells | 5 μM | 30 minutes | Used as an inactive control for KN-93 to study the effect of CaMKII inhibitors on ERK/MAPK cascade activation | Proc Natl Acad Sci U S A. 2005 May 24;102(21):7577-82. | 
| Hippocampal neurons | 2 μM | 24 hours | KN-92, as an inactive analog of KN-93, was used in control experiments, showing that KN-92 did not affect the increase in GluA1 levels | Proc Natl Acad Sci U S A. 2011 Jan 11;108(2):828-33. | 
| Administration | Dosage | Frequency | Description | References | ||
| Rabbit | Isolated heart model | Perfusion | 1 μmol/l | 30 minutes | KN-92 failed to prevent hypokalemia-induced VT/VF | Circulation. 2015 Oct 20;132(16):1528-1537. | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 1.80mL 0.36mL 0.18mL | 9.01mL 1.80mL 0.90mL | 18.02mL 3.60mL 1.80mL | |
| CAS号 | 1135280-28-2 | 
| 分子式 | C24H28ClN2O7PS | 
| 分子量 | 554.98 | 
| SMILES Code | CN(C/C=C/C1=CC=C(C=C1)Cl)CC2=CC=CC=C2NS(=O)(C3=CC=C(C=C3)OC)=O.OP(O)(O)=O | 
| MDL No. | MFCD24369012 | 
| 别名 | |
| 运输 | 蓝冰 | 
| InChI Key | XRQHWVVDNMJDEQ-IPZCTEOASA-N | 
| Pubchem ID | 16219540 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, room temperature | 
| 溶解方案 | 请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 
 
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