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KN-93

KN-93

产品编号 T2697   CAS 139298-40-1

KN-93是 Ca2+/钙调蛋白依赖性激酶 II (CaMKII) 的选择性抑制剂,Ki 为370 nM,可竞争性阻断 CaM 与激酶的结合。

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KN-93 Chemical Structure
KN-93, CAS 139298-40-1
规格 价格/CNY 货期 数量
1 mg ¥ 395 现货
2 mg ¥ 588 现货
5 mg ¥ 878 现货
10 mg ¥ 1,220 现货
25 mg ¥ 2,730 现货
50 mg ¥ 3,660 现货
100 mg ¥ 5,220 现货
1 mL * 10 mM (in DMSO) ¥ 986 现货
其他形式的 KN-93:
产品目录号及名称: KN-93 (T2697)
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纯度: 99.78%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase.
靶点活性 CaMKII:370 nM. (Ki)
体外活性 95% of cells are arrested in G1 after 2 days of KN-93 treatment. G1 arrest is reversible; 1 day after KN-93 release, a peak of cells had progressed into S and G2-M. KN-93 also blocks cell growth stimulated by basic fibroblast growth factor, platelet-derived growth factor-BB, epidermal growth factor, and insulin-like growth factor-1 in NIH 3T3 fibroblasts[1]. KN-93 inhibits the H+, K+-ATPase activity but strongly dissipates the proton gradient formed in the gastric membrane vesicles and reduces the volume of luminal space[2]. KN-93 (0.5 μM) prevents increased LV developed pressure during action potential prolongation and early afterdepolarizations. Ca2+-independent CaM kinase activity is increased during early afterdepolarizations and this increase is prevented by KN-93[3]. KN-93 (10 μM )significantly inhibits the activation of CaMKII/NF-κB signaling induced by elevated glucose, and subsequently decreases the expression of VEGF, iNOS and ICAM-1 in Müller cells[4].
体内活性 KN-93 (1 mg/kg/day, i.p.) inhibits retinal vascular leakage induced by diabetes as well as suppresses phosphorylation of CaMKII and NF-κB in diabetic retina[4].
激酶实验 Cells are grown on 12-mm diameter glass coverslips in DMEM 100% serum and various concentrations of KN-93 or KN-92. After 0, 1, 2, and 3 days of culture in the presence of drug, coverslips are removed from culture, rinsed once in PBS, and then submerged in 100% methanol at -20°C for 3 min. Fixed cells are stored in PBS until staining using the TUNEL assay. Cells are overlaid on 20 μL PBS/1 mg/mL BSA for 30 min, rinsed in PBS, and then overlaid on 20 μL containing 100 mM sodium cacodylate (pH 6.8), 1 mM CoCl2, 0.1 mM DTT, 0.1 mg/mL BSA, 20 μM fluorescein-12-dUTP, and 0.1 unit/μL terminal transferase at 37°C for 60 min. Coverslips are rinsed in PBS twice, mounted on slides, and photographed using an OLYMPUS BX5O epifluorescent microscope using a UPLAN APO 40X oil immersion objective.
细胞实验 KN-93 is dissolved in DMSO. Cell viability is assessed by the 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assay. Briefly, Müller cells are seeded at a density of 10×104 cells per well in 96-well plates and cultured until sub-confluence. Next, cells are treated with curcumin for 24 h before incubation with MTT (5 mg/mL) at 37°C in 5% CO2 atmosphere for 4 h. The culture medium is then removed, and the formazan formed in the reaction is dissolved in 150 μL DMSO. The optical density of the solution is measured at 490 nm using a multifunctional microplate reader. Cell viability in each well is presented as a percentage of the control (vehicle-treated group).
分子量 501.04
分子式 C26H29ClN2O4S
CAS No. 139298-40-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: >10 mM

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9958 mL 9.9792 mL 19.9585 mL 49.8962 mL
5 mM 0.3992 mL 1.9958 mL 3.9917 mL 9.9792 mL
10 mM 0.1996 mL 0.9979 mL 1.9958 mL 4.9896 mL

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参考文献

1. Tombes RM, et al. G1 cell cycle arrest and apoptosis are induced in NIH 3T3 cells by KN-93, an inhibitor of CaMK (the multifunctional Ca2+/CaM kinase). Cell Growth Differ. 1995 Sep;6(9):1063-70. 2. Mamiya N, et al. Inhibition of acid secretion in gastric parietal cells by the Ca2+/calmodulin-dependent protein kinase II inhibitorKN-93. Biochem Biophys Res Commun. 1993 Sep 15;195(2):608-15. 3. Anderson ME, et al. KN-93, an inhibitor of multifunctional Ca++/calmodulin-dependent protein kinase, decreases early afterdepolarizations in rabbit heart. J Pharmacol Exp Ther. 1998 Dec;287(3):996-1006. 4. Li J, et al. Curcumin Attenuates Retinal Vascular Leakage by Inhibiting Calcium/Calmodulin-Dependent Protein Kinase II Activity in Streptozotocin-Induced Diabetes. Cell Physiol Biochem. 2016;39(3):1196-208. 5. Pan X, Li R, Guo H, et al. Dihydropyridine Calcium Channel Blockers Suppress the Transcription of PD-L1 by Inhibiting the Activation of STAT1[J]. Frontiers in Pharmacology. 2021, 11: 2233. 6. Xuexian Fang, Hao Wang, Dan Han, Enjun Xie, Xiang Yang, Jiayu Wei, Shanshan Gu et al. Ferroptosis as a target for protection against cardiomyopathy [J]. Proceedings of the National Academy of Sciences of the United States of America . 2019 Feb 12;116(7):2672-2680.

文献引用

1. Xuexian Fang, Hao Wang, Dan Han, Enjun Xie, Xiang Yang, Jiayu Wei, Shanshan Gu et al. Ferroptosis as a target for protection against cardiomyopathy. Proceedings of the National Academy of Sciences of the United States of America. 2019 Feb 12;116(7):2672-2680. 2. Zheng Q, Zou Y, Teng P, et al. Mechanosensitive Channel PIEZO1 Senses Shear Force to Induce KLF2/4 Expression via CaMKII/MEKK3/ERK5 Axis in Endothelial Cells. Cells. 2022, 11(14): 2191 3. Pan X, Li R, Guo H, et al. Dihydropyridine Calcium Channel Blockers Suppress the Transcription of PD-L1 by Inhibiting the Activation of STAT1. Frontiers in Pharmacology. 2021 Jan 13;11:539261. doi: 10.3389/fphar.2020.539261. eCollection 2020. 4. Jiang Q, Li Y, Mao R, et al.AaCaMKs Positively Regulate Development, Infection Structure Differentiation and Pathogenicity in Alternaria alternata, Causal Agent of Pear Black Spot.International Journal of Molecular Sciences.2023, 24(2): 1381. 5. Yin Z, Zhang J, Zhao M, et al.Maresin‐1 ameliorates hypertensive vascular remodeling through its receptor LGR6.MedComm.2024, 5(3): e491.
Torin 1 Quercitrin Streptozocin Deferoxamine Mesylate Linifanib Lup-20(29)-en-28-oic acid Sitagliptin Ginkgolide K

相关化合物库

该产品包含在如下化合物库中:
活性脂质化合物库 自噬库 NO PAINS 化合物库 抑制剂库

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
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第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

KN-93 139298-40-1 Autophagy Neuroscience CaMK Inhibitor KN93 Calmodulin-dependent protein kinases Calmodulin-dependent kinases inhibit KN 93 inhibitor

 

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