KN-93 hydrochloride
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Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
KN-93 hydrochloride是有效的Ca2+/钙调蛋白依赖性蛋白激酶II(CaMK II)抑制剂,其Ki值为0.37 μM[1].
KN-93是一种CaMK II抑制剂.KN-93与CaMK II的钙调蛋白结合位点竞争而发挥作用,其IC50值为370 nM.在离体胃壁细胞中,KN-93有效抑制氨甲酰胆碱与组胺引起的胃酸分泌,其IC50值分别为0.15 μM和0.3 μM.KN-93也抑制毛喉素诱导的氨基比林摄取,其IC50值为0.6 μM.据发现,KN-93对H+/K+-ATP酶也显效.10 μM KN-93与20 μM KN-93分别抑制26%和35%的酶活性.此外,KN-93能促进C型失活,从而在细胞外阻断Kv通道[1,2].
参考文献：
[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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 537.5 |
| Cas No. | 1956426-56-4 |
| Formula | C26H30Cl2N2O4S |
| Solubility | ≥26.9 mg/mL in DMSO; insoluble in EtOH; ≥5.51 mg/mL in H2O |
| Chemical Name | (E)-N-(2-(((3-(4-chlorophenyl)allyl)(methyl)amino)methyl)phenyl)-N-(2-hydroxyethyl)-4-methoxybenzenesulfonamide hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | O=S(C1=CC=C(OC)C=C1)(N(CCO)C2=CC=CC=C2CN(C)C/C=C/C3=CC=C(Cl)C=C3)=O.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]： | |
|
细胞系 |
NIH 3T3成纤维细胞 |
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溶解方法 |
在DMSO中的溶解度大于10 mM。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应条件 |
24-72 h，24 μM |
|
应用 |
KN-93是钙离子/钙调蛋白依赖性蛋白激酶II（CaMK-II）的抑制剂。它以剂量依赖的方式抑制成纤维细胞CaMK-II的活性及细胞生长，将细胞可逆地阻滞在G1期，诱导细胞凋亡。 |
| 动物实验[2]: | |
|
动物模型 |
8-24周龄的CaMKIV转基因小鼠 |
|
剂量 |
10-30 μmol/kg，腹腔注射 |
|
应用 |
和野生型小鼠比起来，在CaMKIV转基因小鼠里KN-93能够显著抑制异丙肾上腺素诱导的心律失常，表明在心肌肥厚的小鼠模型里CaMKII是一个心律失常分子。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
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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]. Wu Y, Temple J, Zhang R, et al. Calmodulin kinase II and arrhythmias in a mouse model of cardiac hypertrophy[J]. Circulation, 2002, 106(10): 1288-1293. |
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质量控制和MSDS
- 批次:
化学结构
