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Submit ReviewNH 125 is an eukaryotic elongation factor 2 (eEF-2) kinase (CaMK III) inhibitor (IC50 = 60 nM) that displays 125-fold, > 1300-fold and > 1500-fold selectivity over PKC, PKA and CaMK II respectively. Decreases the viability of a variety of cancer cell lines (IC50 values are 0.7 - 4.8 μM) and blocks G1/S cell cycle progression. Shown to induce eEF-2 phosphorylation in cancer cells. Also an effective antibacterial agent; inhibits histidine protein kinase in vitro (IC50 = 6.6 μM) and in vivo.
分子量 | 524.56 |
公式 | C27H45IN2 |
储存 | Desiccate at -20°C |
CAS Number | 278603-08-0 |
PubChem ID | 10436839 |
InChI Key | RVWOHCBHAGBLLT-UHFFFAOYSA-M |
Smiles | CC1=[N+](CCCCCCCCCCCCCCCC)C=CN1CC2=CC=CC=C2.[I-] |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 52.46 | 100 | |
ethanol | 39.34 | 75 |
以下数据基于产品分子量 524.56。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.91 mL | 9.53 mL | 19.06 mL |
5 mM | 0.38 mL | 1.91 mL | 3.81 mL |
10 mM | 0.19 mL | 0.95 mL | 1.91 mL |
50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
参考文献是支持产品生物活性的出版物。
Yamamoto et al (2001) Antibacterial agents that inhibit histidine protein kinase YycG of Bacillus subtilis. Biosci.Biotechnol.Biochem. 65 2306 PMID: 11758928
Arora et al (2003) Identification and characterization of an inhibitor of eukaryotic elongation factor 2 kinase against human cancer cell lines. Cancer Res. 63 6894 PMID: 14583488
Arora et al (2004) P-glycoprotein mediates resistance to histidine kinase inhibitors. Mol.Pharmacol. 66 460 PMID: 15322237
Chen (2011) 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. 286 43951 PMID: 22020937
If you know of a relevant reference for NH 125, please let us know.
关键词: NH 125, NH 125 supplier, CaM, kinase, III, CAMK, eEF-2, inhibitors, inhibits, Histidine, protein, kinases, Calmodulin-Activated, calmodulin-dependent, Protein, NH125, Kinase, Other, Kinases, 3439, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 NH 125 的部分引用包括:
Kim et al (2015) Identification of an Antimicrobial Agent Effective against Methicillin-Resistant Staphylococcus aureus Persisters Using a Fluorescence-Based Screening Strategy. PLoS One 10 e0127640 PMID: 26039584
Xu et al (2017) Neurons secrete miR-132-containing exosomes to regulate brain vascular integrity. Cell Res 27 882 PMID: 28429770
Francis et al (2013) Mechanistic insight into inhibition of two-component system signaling. Medchemcomm 4 269 PMID: 23336064
Cheng et al (2013) Integrated regulation of autophagy and apoptosis by EEF2K controls cellular fate and modulates the efficacy of curcumin and vel. against tumor cells. Autophagy 9 208 PMID: 23182879
Yi et al (2013) Inhibition of elongation factor-2 kinase augments the antitumor activity of Temozolomide against glioma. PLoS One 8 e81345 PMID: 24303044
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