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CAS No.: 278603-08-0

NH125 Catalog No. CSN16664

Synonyms: NH125

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

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生物活性

实验方案

技术信息

生物活性

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].
动物研究
剂量
Mice: 1 mg/kg^[3] (i.p.); 25 mg/kg^[4] (i.v.)

给药途径
i.p., i.v.
参考文献

动物研究
剂量	Mice: 1 mg/kg^[3] (i.p.); 25 mg/kg^[4] (i.v.)
给药途径	i.p., i.v.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9063 mL
- 9.5317 mL
- 19.0634 mL
- 5 mM
- 0.3813 mL
- 1.9063 mL
- 3.8127 mL
- 10 mM
- 0.1906 mL
- 0.9532 mL
- 1.9063 mL

技术信息

CAS号

278603-08-0

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H45IN2

运输

蓝冰

分子量

524.56

别名

NH125

溶解度

DMSO	88.0 mg/mL (167.8 mM) warming
Water	insoluble

动物实验配方

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NH125 Catalog No. CSN16664

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