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NH125
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
NH125图片
CAS NO:278603-08-0
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
2mg电议
5mg电议

产品介绍
NH125 是一种有效且选择性的真核延伸因子 2 激酶 (eEF-2K/CaMKIII) 抑制剂，也可诱导 eEF2 磷酸化，对 eEF-2K 的 IC50 为 60 nM。
Cas No.278603-08-0
化学名1-benzyl-3-hexadecyl-2-methylimidazol-1-ium;iodide
Canonical SMILESCCCCCCCCCCCCCCCCN1C=C[N+](=C1C)CC2=CC=CC=C2.[I-]
分子式C27H45IN2
分子量524.56
溶解度≥ 25.9mg/mL in DMSO
储存条件Store at -20° C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

NH125 is a selective inhibitor of eEF-2 with IC50 value of 60 nM [1].

Eukaryotic elongation factor-2 kinase (eEF-2 kinase or eEF-2K), also known as calcium/calmodulin-dependent eukaryotic elongation factor 2 kinase (CaMKIII) is a highly conserved protein kinase in the calmodulin-mediated signaling pathway and plays an important role in regulating protein [1, 2].

NH125 is a potent eEF-2 inhibitor and has 1000- to >100000-fold more potent against eEF-2 compared with PKC, PKA and CamK-II. When tested with a panel of 10 cancer cell lines (C6, T98-G, U-138 MG, and so forth), NH125 treatment inhibited cell viability with IC50 value ranges from 0.7 to 4.8 μM. And NH125 decreased the cellular content of p-eEF-2 without affecting total content eEF-2 and arrested cell in G0-G1 phase in C6 glioma cells [1]. In HUVECs, NH125 treatment inhibited TNF-α-induced inflammatory responses at the dose of 1μM/L [3]. When tested with a panel of human cancer cell lines (glioblastoma, breast cancer, and so on), NH125 sensitized cells at the dose of 0.25 μM which thus reinforced the efficacy of ER stress-inducing drug by inhibiting eEF-2 [2].

In spontaneously hypertensive-SHR (10 wk old) rat model, administration of NH125 (500 μg·kg–1·day–1) for 6 weeks resulted in significant reduction SBP, reduced the increased expression of VCAM-1 and E-selectin and inhibited the increased ROS production and wall thickness in SHR [3].

It is also reported that NH125 inhibited protein kinase C (PKC), protein kinase A (PKA), and calmodulin-dependent kinase II (CamK-II) with IC50 value of 7.5 μM, 80 μM and >100 μM, respectively [1].

References:
[1].  Arora, S., et al., Identification and characterization of an inhibitor of eukaryotic elongation factor 2 kinase against human cancer cell lines. Cancer Res, 2003. 63(20): p. 6894-9.
[2].  Cheng, Y., et al., Integrated regulation of autophagy and apoptosis by EEF2K controls cellular fate and modulates the efficacy of curcumin and velcade against tumor cells. Autophagy, 2013. 9(2): p. 208-19.
[3].  Usui, T., et al., Eukaryotic elongation factor 2 kinase regulates the development of hypertension through oxidative stress-dependent vascular inflammation. Am J Physiol Heart Circ Physiol, 2013. 305(5): p. H756-68.