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NH125 {[allProObj[0].p_purity_real_show]}

货号:A261079

NH125 is a selective eEF-2 kinase inhibitor with IC50 of 60 nM, also a potent histidine kinase inhibitor.

NH125 化学结构 CAS号:278603-08-0
NH125 化学结构
CAS号:278603-08-0
NH125 3D分子结构
CAS号:278603-08-0
NH125 化学结构 CAS号:278603-08-0
NH125 3D分子结构 CAS号:278603-08-0
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NH125 纯度/质量文件 产品仅供科研

货号:A261079 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 CaMKII CaMKIII CaMKKα CaMKKβ PKD 其他靶点 纯度
KN-62 +

CaMKII, Ki: 0.9 μM

98%
KN-93 ++

CaMKII, Ki: 0.37 μM

98%
NH125 +++

eEF-2 kinase, IC50: 60 nM

99%+
STO-609 ++

CaM-KKα, Ki: 0.25 μM

++++

CaM-KKβ, Ki: 47 nM

98%
CID755673 +++

PKD2, IC50: 227 nM

PKD1, IC50: 180 nM

99%+
CRT0066101 2HCl ++++

PKD2, IC50: 2 nM

PKD1, IC50: 1 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

NH125 生物活性

靶点
  • CaMKIII

    eEF-2 kinase, IC50:60 nM

描述 H125 is a selective eEF2K inhibitor with IC50 value of 60nM in vitro. It blocked the phosphorylation of eEF-2 in intact C6 glioma cells at 1μM post 12h. It decreased the viability of 10 cancer cell lines from rat glioblastoma, human glioblastoma, human ovarian carcinoma, human cervical carcinoma, human prostate carcinoma, human ovarian carcinoma and human breast carcinoma with IC50 values ranging from 0.7 to 4.7μM[3]. On the contrary, some study showed that NH125 was more correlated with induction of eEF2 phosphorylation than inhibition of eEF2K[4].

NH125 动物研究

Dose Mice: 1 mg/kg[3] (i.p.); 25 mg/kg[4] (i.v.)
Administration i.p., i.v.

NH125 参考文献

[1]Arora S, Yang JM, et al. Identification and characterization of an inhibitor of eukaryotic elongation factor 2 kinase against human cancer cell lines. Cancer Res. 2003 Oct 15;63(20):6894-9.

[2]Chen Z, Gopalakrishnan SM, et al. 1-Benzyl-3-cetyl-2-methylimidazolium iodide (NH125) induces phosphorylation of eukaryotic elongation factor-2 (eEF2): a cautionary note on the anticancer mechanism of an eEF2 kinase inhibitor. J Biol Chem. 2011 Dec 23;286(51):43951-8.

[3]Arora S, Yang JM, Kinzy TG, Utsumi R, Okamoto T, Kitayama T, Ortiz PA, Hait WN. Identification and characterization of an inhibitor of eukaryotic elongation factor 2 kinase against human cancer cell lines. Cancer Res. 2003 Oct 15;63(20):6894-9. PMID: 14583488.

[4]Chen Z, Gopalakrishnan SM, Bui MH, Soni NB, Warrior U, Johnson EF, Donnelly JB, Glaser KB. 1-Benzyl-3-cetyl-2-methylimidazolium iodide (NH125) induces phosphorylation of eukaryotic elongation factor-2 (eEF2): a cautionary note on the anticancer mechanism of an eEF2 kinase inhibitor. J Biol Chem. 2011 Dec 23;286(51):43951-43958. doi: 10.1074/jbc.M111.301291. Epub 2011 Oct 21. PMID: 22020937; PMCID: PMC3243513.

NH125 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.53mL

1.91mL

0.95mL

19.06mL

3.81mL

1.91mL

NH125 技术信息

CAS号278603-08-0
分子式C27H45IN2
分子量 524.564
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 50 mg/mL(95.32 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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