KN-92 hydrochloride
(Synonyms: KN-92盐酸盐,KN 92 hydrochloride;KN92 hydrochloride) 目录号 : GC15988
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。
Cas No.:1431698-47-3
Sample solution is provided at 25 µL, 10mM.
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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]。
| Cell experiment[1]: | |
|
Cell lines |
NIH 3T3 fibroblasts |
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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. | |
| Cas No. | 1431698-47-3 | SDF | |
| 别名 | 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 | ||
| Canonical 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 |
| 溶解度 | ≥ 24.65 mg/mL in DMSO, ≥ 11.73 mg/mL in EtOH with ultrasonic and warming | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0265 mL | 10.1327 mL | 20.2655 mL |
| 5 mM | 405.3 μL | 2.0265 mL | 4.0531 mL |
| 10 mM | 202.7 μL | 1.0133 mL | 2.0265 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet