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CAS No.: 1431698-47-3

KN-92 HCl Catalog No. CSN17850

Synonyms: KN-92 (hydrochloride);KN-92

KN-92 HCl a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM).

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技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0266 mL
- 10.1328 mL
- 20.2657 mL
- 5 mM
- 0.4053 mL
- 2.0266 mL
- 4.0531 mL
- 10 mM
- 0.2027 mL
- 1.0133 mL
- 2.0266 mL

技术信息

CAS号

1431698-47-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H26Cl2N2O3S

运输

蓝冰

分子量

493.45

别名

KN-92 (hydrochloride);KN-92

溶解度

DMSO	50.0 mg/mL (101.3 mM)

动物实验配方

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