KN-93 hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
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 |
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。 |
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. |
质量控制和MSDS
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