KN-92 hydrochloride

目录号: GC15988纯度: >99.50%同义词: KN-92盐酸盐,KN 92 hydrochloride;KN92 hydrochloride
KN-92 hydrochloride是KN-93的非活性类似物,可通过结构修饰转化为KN-93。

KN-92 hydrochloride
Cas No.: 1431698-47-3
规格价格库存数量操作
1mg¥280.00现货
1
5mg¥910.00现货
1
10mg¥1,540.00现货
1
25mg¥2,590.00现货
1
50mg¥3,850.00现货
1

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产品描述 Description

KN-92 hydrochloride is an inactive analogue of KN-93 and can be converted to KN-93 by modification[1]. KN-92 hydrochloride has a weak ionic current inhibition activity and can inhibit some Kv channels[2]. KN-92 hydrochloride is often used as a negative control to elucidate the inhibitory activity of KN-93 on CaMKII in mammalian eggs[3]. KN-92 hydrochloride can be used as a model compound to develop a new HPLC-MS technology for the identification of related substances[4].

References:
[1] Bruno C, Lentini G, Catalano A, et al. Microwave-Assisted Synthesis of KN-93, a Potent and Selective Inhibitor of Ca2+/Calmoduline-Dependent Protein Kinase II[J]. Synthesis, 2010, 2010(24): 4193-4198.
[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[J]. The Journal of pharmacology and experimental therapeutics, 2006, 317(1): 292-299.
[3] Tatone C, Iorio R, Francione A, et al. Biochemical and biological effects of KN-93, an inhibitor of calmodulin-dependent protein kinase II, on the initial events of mouse egg activation induced by ethanol[J]. Reproduction, 1999, 115(1): 151-157.
[4] Erwin T, Rekulapally S P, Abraham T S, et al. A non-radioactive in vitro CaMKII activity assay using HPLC-MS[J]. Journal of Pharmacological and Toxicological Methods, 2018, 94: 64-70.

KN-92 hydrochloride是KN-93的非活性类似物,可通过结构修饰转化为KN-93[1]。KN-92 hydrochloride具有较弱的离子电流抑制活性,能够抑制部分Kv通道[2]。KN-92 hydrochloride常作为阴性对照,用于阐明KN-93对哺乳动物卵细胞中CaMKII的抑制活性[3]。KN-92 hydrochloride可作为模型化合物,用于开发鉴定相关物质的新型HPLC-MS技术[4]

实验参考方法 Experimental Reference Method

Cell experiment[1]:

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

72 h, 4-24 μM

Applications

KN-92 is an inactive derivative of KN-93. KN-92 is usually used as a control in studies to elucidate the effect of KN-93. KN-93 inhibits fibroblast CaMK-II activity and cell growth, whereas KN-92 had no effect on CaMK-II activity or cell growth.

Animal experiment [2]:

Animal models

AC3-I and AC3-C transgenic mice

Dosage form

20 μmol/kg, intraperitoneal

Application

Treatment with KN-93 in WT mice resulted in a dose-dependent improvement in left ventricular function compared to WT mice treated with KN-92. Surviving myocytes from infarcted wild-type mice without treatment or treated with control drug KN-92 exhibited severely disordered Ca2+ homeostasis. In contrast, Ca2+ homeostasis was preserved after myocardial infarction in wild-type mice treated with KN-93.

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.

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.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
1431698-47-3
同义词
KN-92盐酸盐,KN 92 hydrochloride;KN92 hydrochloride
化学名
(E)-N-(2-(((3-(4-chlorophenyl)allyl)(methyl)amino)methyl)phenyl)-4-methoxybenzenesulfonamide hydrochloride
SMILES
ClC1=CC=C(/C=C/CN(C)CC2=CC=CC=C2NS(C3=CC=C(OC)C=C3)(=O)=O)C=C1.Cl
分子式
C24H26Cl2N2O3S
分子量
493.45 g/mol
溶解性
≥ 24.65 mg/mL in DMSO, ≥ 11.73 mg/mL in EtOH with ultrasonic and warming
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol