NH125 |
| Catalog No.GC13793 |
Selective eEF-2 kinase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 278603-08-0
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 278603-08-0 | SDF | |
| Chemical Name | 1-benzyl-3-hexadecyl-2-methylimidazol-1-ium;iodide | ||
| Canonical SMILES | CCCCCCCCCCCCCCCCN1C=C[N+](=C1C)CC2=CC=CC=C2.[I-] | ||
| Formula | C27H45IN2 | M.Wt | 524.56 |
| Solubility | ≥ 25.9mg/mL in DMSO | Storage | Store at -20° C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9064 mL | 9.5318 mL | 19.0636 mL |
| 5 mM | 0.3813 mL | 1.9064 mL | 3.8127 mL |
| 10 mM | 0.1906 mL | 0.9532 mL | 1.9064 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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