KN-62
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-62(1-[N,O-bis-(5-isoquinolinesulphonyl)-N-methyl-L-tyrosy]-4-phenylpiperazine)是一种高选择性的钙依赖性钙调蛋白激酶II(CAMKII)抑制剂,与CAMKII的钙调蛋白结合位点相结合,因而不能抑制其它类的钙调蛋白敏感激酶。在以前的研究中,KN-62通过质膜上L型Ca2+通道阻断Ca2+内流,抑制由内在薄层(HIT)细胞的异质连接所调节的胰岛素分泌和斯钙素-1(STC-1)肠内分泌细胞中胆囊收缩素的分泌。KN-62还抑制骨骼肌中胰岛素和缺氧刺激的葡萄糖转运活性,分别抑制了46%和40%。
参考文献:
Joseph T. Brozinick, Jr., Thomas H. Reynolds, David Dean, Gregory Cartee and Samuel W. Cushman. 1-[N,O-bis-(5-isoquinolinesulphonyl)-N-methyl-L-tyrosy]-4-phenylpiperazine (KN-62), an inhibitor of calcium-dependent camodulin protein kinase II, inhibits both insulin- and hypoxia-stimulated glucose transport in skeletal muscle. Biochem. J. (1999) 339, 533-540
Erik S. Schweitzer, Michael J. Sanderson and C. G. Wasterlain. Inhibition of regulated catecholamine secretion from PC12 cells by the Ca2+/calmodulin kinase II inhibitor KN-62. Journal of Cell Science 108. 2619-2628 (1995)
Physical Appearance | A solid |
Storage | Desiccate at -20°C |
M.Wt | 721.9 |
Cas No. | 127191-97-3 |
Formula | C38H35N5O6S2 |
Solubility | ≥36.1 mg/mL in DMSO; insoluble in H2O; ≥15.88 mg/mL in EtOH with ultrasonic |
Chemical Name | [4-[(2S)-2-[isoquinolin-5-ylsulfonyl(methyl)amino]-3-oxo-3-(4-phenylpiperazin-1-yl)propyl]phenyl] isoquinoline-5-sulfonate |
SDF | Download SDF |
Canonical SMILES | CN(C(CC1=CC=C(C=C1)OS(=O)(=O)C2=CC=CC3=C2C=CN=C3)C(=O)N4CCN(CC4)C5=CC=CC=C5)S(=O)(=O)C6=CC=CC7=C6C=CN=C7 |
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。 |
激酶实验 [1]: | |
激酶实验 |
采用标准2分钟试验 (100 μL) 测定CaMKII总激酶活性。上述试验于30 °C下进行,反应体系包含35 mM HEPES,10 mM MgCl2,1 mM CaCl2,10 μg鸡胃肌球蛋白(20 kD 轻链),0.1 μM钙调蛋白以及10 μM [γ-33]ATP。加入1 mL 10%三氯乙酸终止上述激酶反应。 |
细胞实验 [2]: | |
细胞系 |
K562细胞 |
制备方法 |
在DMSO中的溶解度大于36.1 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
1、2、5或10 μM;24或48小时 |
实验结果 |
KN-62呈剂量依赖性地抑制K562细胞生长。给予10 μM KN-62,2天后,63% K562细胞受抑制。流式细胞仪分析结果显示KN-62(10 μM,24小时)使K562细胞停滞于S期。免疫印迹实验表明CaMKII在上述K562细胞中受抑制。 |
References: [1]. Tokumitsu H, Chijiwa T, Hagiwara M, Mizutani A, Terasawa M, Hidaka H. KN-62, 1-[N,O-bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazi ne, a specific inhibitor of Ca2+/calmodulin-dependent protein kinase II. J Biol Chem. 1990 Mar 15;265(8):4315-20. [2]. Minami H, Inoue S, Hidaka H. The effect of KN-62, Ca2+/calmodulin dependent protein kinase II inhibitor on cell cycle. Biochem Biophys Res Commun. 1994 Feb 28;199(1):241-8. |
描述 | KN-62是一种有效的和特异性的Ca2+/钙调蛋白依赖性蛋白激酶II(CaMKII)抑制剂,Ki值为0.9 μM。 | |||||
靶点 | Calmodulin protein kinase II | |||||
IC50 | 0.9 μM |
质量控制和MSDS
- 批次: