NH125 |
Catalog No.GC13793
One-Click Copy Product Info
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NH125 is a multitarget active substance and an inhibitor of several members of the histidine protein kinase family. NH125 can inhibit the activity of eukaryotic elongation factor-2 kinase (eEF-2K) with an IC50 of 60nM .
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 multitarget active substance and an inhibitor of several members of the histidine protein kinase family[1]. NH125 can inhibit the activity of eukaryotic elongation factor-2 kinase (eEF-2K) with an IC50 of 60nM [2]. NH125 can also target and inhibit the two-component signal transduction system in bacteria, exerting antibacterial effects[3]. NH125 can reduce the expression of the RNA-binding protein CPEB3 to increase the level of synaptic GluA2[4].
In vitro, pre-treatment of Staphylococcus aureus strain Newman with NH125 (41–298μM) for 1 hour, followed by cultivation for 24 hours in the presence of sub-lethal doses of cell wall-targeting antibiotics (Oxacillin at 0.5MIC or Vancomycin at 0.5MIC), significantly enhanced the inhibitory effects of the antibiotics on bacterial growth and reduced the expression levels of antibiotic resistance-related genes (vraSR, pbpB, and blaZ)[5]. Co-treatment of tumor cells with NH125 (0.25μM) and endoplasmic reticulum (ER) stress inducers (Curcumin at 5-50μM or Velcade at 25-800nM) for 48 hours significantly enhanced the cytotoxicity of the ER stress inducers against tumor cells and promoted apoptosis compared to treatment with the ER stress inducers alone[6].
In vivo, NH125 (1mg/kg) was administered intraperitoneally once daily to mice with LPS-induced depression. NH125 reduced the levels of pro-inflammatory cytokines and increased the immobility time of the mice[7]. NH125 (1mg/kg) was also administered intraperitoneally once daily to SARM1 knockout (SARM1KO) mice for 3 consecutive days. NH125 significantly improved depressive-like behaviors in SARM1KO mice, reducing immobility time, increasing sucrose preference, and restoring synaptic protein levels while increasing dendritic spine density[8].
References:
[1] Devkota AK, Tavares CD, Warthaka M, et al. Investigating the kinetic mechanism of inhibition of elongation factor 2 kinase by NH125: evidence of a common in vitro artifact. Biochemistry. 2012 Mar 13;51(10):2100-12.
[2] Arora S, Yang JM, Kinzy TG, 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.
[3] Yamamoto K, Kitayama T, Ishida N, et al. Identification and characterization of a potent antibacterial agent, NH125 against drug-resistant bacteria. Biosci Biotechnol Biochem. 2000 Apr;64(4):919-23.
[4] Bender CL, Yang Q, Sun L, et al. NH125 reduces the level of CPEB3, an RNA binding protein, to promote synaptic GluA2 expression. Neuropharmacology. 2016 Feb;101:531-7.
[5] Bhattarai S, Marsh L, Knight K, et al. NH125 Sensitizes Staphylococcus aureus to Cell Wall-Targeting Antibiotics through the Inhibition of the VraS Sensor Histidine Kinase. Microbiol Spectr. 2023 Jun 15;11(3):e0486122.
[6] Cheng Y, Ren X, Zhang 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 Feb 1;9(2):208-19.
[7] Li W, Ali T, Zheng C, et al. Fluoxetine regulates eEF2 activity (phosphorylation) via HDAC1 inhibitory mechanism in an LPS-induced mouse model of depression. J Neuroinflammation. 2021 Feb 1;18(1):38.
[8] Li W, Zhu W, Chen J, et al. SARM1 deficiency induced depressive-like behavior via AMPKα/p-eEF2 axis to synapse dysfunction. Neuropharmacology. 2025 Jan 1;262:110206.
| Cell experiment [1]: | |
Cell lines | T98G and LN-229 cells (human glioblastoma cell lines) |
Preparation Method | T98G, LN-229 cells were cultured in Ham's F-DMEM (10:1) medium supplemented with 10% fetal bovine serum at 37°C, 5% CO₂. Cells were treated with of NH125 (0.25μM) and Curcumin (5-50μM) or Velcade (25-800nM) for 48 hours. |
Reaction Conditions | 0.25μM; 48h |
Applications | NH125 significantly increased the cytotoxicity of Curcumin and Velcade against T98G and LN-229 cells. This suggests that NH125 can enhance the efficacy of these ER stress-inducing anticancer drugs by inhibiting EEF2K-mediated autophagy. |
| Animal experiment [2]: | |
Animal models | C57BL/6J male mice |
Preparation Method | Mice were treated with lipopolysaccharide (LPS) (2mg/kg, intraperitoneally) to induce depression-like behavior. Some mice were also treated with the HDAC1 inhibitor NH125 (1mg/kg, intraperitoneally) to investigate its effects on LPS-induced neuroinflammation and depression. |
Dosage form | 1mg/kg; i.p. |
Applications | NH125 treatment significantly reduced LPS-induced depressive-like behaviors, as evidenced by decreased immobility time in the forced swimming test and increased sucrose preference in the sucrose preference test. NH125 also attenuated LPS-induced neuroinflammation by reducing the expression of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) and NLRP3 inflammasome components. |
References: | |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9064 mL | 9.5318 mL | 19.0636 mL |
| 5 mM | 381.3 μL | 1.9064 mL | 3.8127 mL |
| 10 mM | 190.6 μL | 953.2 μL | 1.9064 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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 saline, 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)