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KN-92 hydrochloride

现货
Catalog No.
A3530
KN-93的无活性衍生物,对照化合物
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 2,650.00
现货
5mg
¥ 2,570.00
现货
10mg
¥ 3,550.00
现货
50mg
¥ 9,360.00
现货
200mg
¥ 21,490.00
现货

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Background

KN-92 is an inactive analog of KN-93. KN-93 is the CaM kinase II inhibitor. [1]

Hearts were treated with the CaM kinase inhibitor KN-93 or the inactive analog KN-92 (0.5 μM) for 10 min before clofilium exposure. Early afterdepolarizations (EADs) were largely inhibited by KN-93 contrasted to KN-92. There were little differences in parameters favoring EADs such as monophasic action potential duration or heart rate in KN-92- or KN-93- treated hearts. CaM kinase activity in situ increased 37% in hearts with EADs compared to hearts without EADs. This increase in CaM kinase activity was prevented by pretreatment with KN-93. [1]

In vitro, KN-93 potently suppressed rabbit myocardial CaM kinase activity (calculated Ki ≤ 2.58 μM), but the inactive analog KN-92 did not (Ki > 100 μM). The actions of KN-93 and KN-92 on ICa and other repolarizing K+currents did not illustrate preferential EAD suppression by KN-93. [1]

Reference:
1.  KN-93, an inhibitor of multifunctional Ca++/calmodulin-dependent protein kinase, decreases early afterdepolarizations in rabbit heart. J Pharmacol Exp Ther. 1998 Dec;287(3):996-1006.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt493.45
Cas No.1431698-47-3
FormulaC24H26Cl2N2O3S
SynonymsKN 92 hydrochloride;KN92 hydrochloride
Solubility≥24.65 mg/mL in DMSO, ≥11.73 mg/mL in EtOH with ultrasonic and warming, <2.61 mg/mL in H2O
Chemical Name(E)-N-(2-(((3-(4-chlorophenyl)allyl)(methyl)amino)methyl)phenyl)-4-methoxybenzenesulfonamide hydrochloride
SDFDownload SDF
Canonical SMILESClC1=CC=C(/C=C/CN(C)CC2=CC=CC=C2NS(C3=CC=C(OC)C=C3)(=O)=O)C=C1.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

NIH 3T3成纤维细胞

溶解方法

在DMSO中的溶解度大于10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

72 h,4-24 μM

应用

KN-92是KN-93的无活性衍生物,在KN-93作用研究中通常用作对照。KN-93抑制成纤维细胞CaMK-II的活性及细胞生长,然而KN-92对CaMK-II活性和细胞生长都没有作用。

动物实验[2]:

动物模型

AC3-I和AC3-C转基因小鼠

剂量

20 μmol/kg,腹腔注射

应用

和KN-92比起来,KN-93处理导致野生型小鼠左心室功能以剂量依赖的方式改善。从未处理或对照药物KN-92处理的梗塞野生型小鼠得到的存活肌细胞钙稳态严重失调,然而,KN-93处理的野生型小鼠心肌梗塞后依然维持钙稳态。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Tombes R M, Grant S, Westin E H, et al. G1 cell cycle arrest and apoptosis are induced in NIH 3T3 cells by KN-93, an inhibitor of CaMK-II (the multifunctional Ca2+/CaM kinase)[J]. Cell growth & differentiation: the molecular biology journal of the American Association for Cancer Research, 1995, 6(9): 1063.

[2]. Zhang R, Khoo M S C, Wu Y, et al. Calmodulin kinase II inhibition protects against structural heart disease[J]. Nature medicine, 2005, 11(4): 409-417.

生物活性

Description KN-92 hydrochloride是KN-93的阴性对照。
靶点            
IC50            

质量控制

化学结构

KN-92 hydrochloride