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KN-93 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
KN-93 hydrochloride图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
KN-93 hydrochloride 是一种可渗透细胞的可逆竞争性抑制剂钙调蛋白依赖性激酶 II 型 (CaMKII),Ki 为 370 nM。

Cell lines

NIH 3T3 fibroblasts

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

24-72 h, 24 μM

Applications

KN-93 is an inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMK-II). It inhibits fibroblast CaMK-II activity and cell growth in a dose-dependent manner, reversibly arrests cells in G1 and induces apoptosis.

Animal models

8-24-week-old CaMKIV TG mice

Dosage form

10 to 30 μmol/kg IP

Application

KN-93 significantly suppressed isoproterenol-induced arrhythmias in CaMKIV TG mice compared with isoproterenol-treated WT mice, indicating CaMKII is a proarrhythmic molecule in the mouse model of cardiac hypertrophy.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

KN-93 hydrochloride is a potent inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMK II) with Ki value of 0.37μM [1].

KN-93 is an inhibitor of CaMK II. It exerts its effect by competing for the calmodulin binding site of CaMK II with IC50 value of 370nM. In isolated gastric parietal cells, KN-93 shows a potent inhibition of acid secretion induced by carbachol and histamine with IC50 values of 0.15μM and 0.3μM, respectively. It also inhibits forskolin induced aminopyrine uptake with IC50 value of 0.6μM. KN-93 is also found to have effects on the H+, K+-ATPase. 10μM KN-93 and 20μM KN-93 can inhibit 26% and 35% activity of the enzyme, respectively. Moreover, KN-93 is reported to act as an extracellular blocker of Kv channels through enhancing C-type inactivation [1, 2].

References:
[1] Mamiya N, Goldenring J R, Tsunoda Y, et al. Inhibition of Acid Secretion in Gastric Parietal Cells by the Ca2+/Calmodulin-Dependent Protein Kinase II Inhibitor KN-93. Biochemical and biophysical research communications, 1993, 195(2): 608-615.
[2] Rezazadeh S, Claydon T W, Fedida D. 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 potassium channels. Journal of Pharmacology and Experimental Therapeutics, 2006, 317(1): 292-299.