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KN-92 HCl

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Chemical Structure| 1431698-47-3 同义名 : KN-92 (hydrochloride)
CAS号 : 1431698-47-3
货号 : A105838
分子式 : C24H26Cl2N2O3S
纯度 : 98%
分子量 : 493.446
MDL号 : MFCD25372041
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(101.33 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 CaMKII (Ca2+/calmodulin-dependent protein kinase II), a multi functional protein kinase, is ubiquitously involved in many physiological processes including control of cell cycle, apoptosis, gene expression, and neurotransmission. KN-93, as a membrane permeant compound of CaMKII-selective inhibitor, can intensively prevent CaMK-II activation by antagonizing CaM binding. In contrast to KN-93, KN-92 is a congener of KN-93 without CaM kinase inhibitory activity and has been used as an experimental control. KN-93 inhibited proliferation of LX-2 cells in a dose- and time-dependent manner, but KN-92 was ineffective in blocking cell growth. KN-92 showed little impact on p53 expression, demonstrating that it was KN-93 rather than KN-92 increased p53 expression in a dose-dependent manner[3]. The incidence of EADs (early after-depolarizations) and I(Ca, L) in the hypertrophic cardiomyocytes were evaluated after treatment with different concentrations of KN-92. The incidence of EADs was 10/12 in KN-92 group (0.5 μmol/L). When the drug concentration was increased to 1 μmol/L in KN-92 group, the incidence of EADs remained the same. When the drug concentration was 0.5 μmol/L in KN-92 groups, the peak I(Ca, L) at 0 mV was decreased by (9.4 ± 2.8)% in the hypertrophic cardiomyocytes (P>0.05, n=12). When the drug concentration was increased to 1 μmol/L, the peak I(Ca, L) value was lowered by (13.4 ± 3.7)% (P<0.01, n=12)[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.13mL

2.03mL

1.01mL

20.27mL

4.05mL

2.03mL
参考文献

[1]Rokhlin OW, Guseva NV, et al. KN-93 inhibits androgen receptor activity and induces cell death irrespective of p53 and Akt status in prostate cancer. Cancer Biol Ther. 2010 Feb;9(3):224-35.

[2]An P, Zhu JY, et al. KN-93, a specific inhibitor of CaMKII inhibits human hepatic stellate cell proliferation in vitro. World J Gastroenterol. 2007 Mar 7;13(9):1445-8.

[3]KN-93, a Specific Inhibitor of CaMKII Inhibits Human Hepatic Stellate Cell Proliferation in Vitro

[4]Effects of Calmodulin-Dependent Protein Kinase II Inhibitor, KN-93, on Electrophysiological Features of Rabbit Hypertrophic Cardiac Myocytes