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NH125

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Chemical Structure| 278603-08-0 同义名 : -
CAS号 : 278603-08-0
货号 : A261079
分子式 : C27H45IN2
纯度 : 99%+
分子量 : 524.564
MDL号 : MFCD07370143
存储条件:

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

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:
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].
实验方案
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

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.