A-484954
Based on 9 publication(s) in Google Scholar
A-484954 is a highly selective eukaryotic elongationfactor-2 kinase(eEF2K) inhibitor, with an IC50 of 280 nM.
For research use only. We do not sell to patients.
- Purity: 99.57%
- CAS No.: 142557-61-7
- Formula: C13H15N5O3
- Molecular Weight:289.29
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) A-484954
More- J Exp Med. 2023 Nov 6;220(11):e20230577. [Abstract]
- J Nutr Biochem. 2026 Jun 24:110454. [Abstract]
- Eur J Pharmacol. 2025 May 21:177746. [Abstract]
- Molecules. 2023 Jan 21;28(3):1095. [Abstract]
- Poult Sci. 2026 May 25.
- iScience. 2025 Jul 10;28(8):113085. [Abstract]
- Sports Med Health Sci. 2024 Mar 8;7(1):37-47. [Abstract]
- Mol Genet Genomics. 2026 Jan 31;301(1):26. [Abstract]
- bioRxiv. 2024 Mar 7:2024.03.04.583390. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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Flow Cytometry
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ELISA
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WB
Biological Activity
IC50: 280 nM (eEF2K)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
>100 μM
Compound: Compound 4; A484954
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Antiproliferative activity against human MDA-MB-231 cells assessed as decrease in cell viability after 24 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as decrease in cell viability after 24 hrs by MTT assay
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[PMID: 29202403] |
| MDA-MB-231 | IC50 |
99480 nM
Compound: A-484954
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Antitumor activity against human MDA-MB-231 cells assessed as inhibition of cell viability by measuring inhibition rate measured after 72 hrs by CCK-8 assay relative to control
Antitumor activity against human MDA-MB-231 cells assessed as inhibition of cell viability by measuring inhibition rate measured after 72 hrs by CCK-8 assay relative to control
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[PMID: 39208364] |
| MDA-MB-436 | IC50 |
>100 μM
Compound: Compound 4; A484954
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Antiproliferative activity against human MDA-MB-436 cells assessed as decrease in cell viability after 24 hrs by MTT assay
Antiproliferative activity against human MDA-MB-436 cells assessed as decrease in cell viability after 24 hrs by MTT assay
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[PMID: 29202403] |
A-484954 is a highly selective eEF2K inhibitor with an IC50 value of 280 nM against eEF2K in the enzymatic assay and little activity against a wide panel of serine/threonine and tyrosine kinases. In enzymatic assay, the IC50 value of A-484954 is increased as the concentration of ATP increased but unaffected by increasing concentrations of calmodulin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Long-term A-484954 treatment inhibits MCT-induced increases PA pressure. It is revealed that A-484954 inhibits MCT-induced PA hypertrophy and fibrosis but not impairment of endothelium-dependent and -independent relaxation. Furthermore, A-484954 inhibits MCT-induced NADPH oxidase-1 expression and ROS generation as well as matrix metalloproteinase-2 activation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 142557-61-7
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Appearance Solid
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Molecular Weight 289.29
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Formula C13H15N5O3
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Color White to off-white
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SMILES
O=C(N1CC)N(C2CC2)C3=C(C=C(C(N)=O)C(N)=N3)C1=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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J Exp Med
2023 Nov 6;220(11):e20230577. PMID: 37584653
A-484954 purchased from MedChemExpress. Usage Cited in: J Exp Med. 2023 Nov 6;220(11):e20230577. [Abstract]
CD14+ human monocytes were cultured with KS for indicated time points and treated with DMSO or A-484954 (25 μΜ) for 6 h before sample analysis. Intracellular CXCL10 levels were measured by ELISA.
A-484954 purchased from MedChemExpress. Usage Cited in: J Exp Med. 2023 Nov 6;220(11):e20230577. [Abstract]
CD14+ human monocytes were cultured with KS for indicated time points and treated with DMSO or A-484954 (25 μΜ) for 6 h before sample analysis. The protein levels of p-eEF2 (Thr56) and total eEF2 were detected by Western blotting.
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J Nutr Biochem
2026 Jun 24:110454. PMID: 42342138 -
Eur J Pharmacol
Targeting eEF2K induces oxidative stress and sensitizes cancer cells to ferroptosis induction. [Abstract]2025 May 21:177746. PMID: 40409701
A-484954 purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2025 May 21:177746. [Abstract]
Dose-response curves for HeLa, U2-OS, MCF-7, and MDA-MB-231 cells treated with A484954 for 24 hours were determined using the CCK-8 assay. The IC50 values for all cell lines exceeded 100 μM.
A-484954 purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2025 May 21:177746. [Abstract]
Western blot analysis was used to detect the expression levels of phosphorylated eEF2 (p-eEF2) and total eEF2 in cells treated with 15 μM A484954 for 24 hours.
A-484954 purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2025 May 21:177746. [Abstract]
ROS levels in HeLa, U2-OS, MCF-7, and MDA-MB-231 cells treated with A484954 (15 μM, 24 h) were evaluated using DCFDA staining and flow cytometry.
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Molecules
2023 Jan 21;28(3):1095. PMID: 36770760 -
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iScience
Conditional deletion of TRPC1 channel modulates synaptic plasticity, long term depression, and memory extinction in Fragile X syndrome mice. [Abstract]2025 Jul 10;28(8):113085. PMID: 40777047 -
Sports Med Health Sci
Exercise improves systemic metabolism in a monocrotaline model of pulmonary hypertension. [Abstract]2024 Mar 8;7(1):37-47. PMID: 39649790 -
Mol Genet Genomics
Buparlisib induces eukaryotic elongation factor-2 expression to cause treatment failure for lung cancer cells. [Abstract]2026 Jan 31;301(1):26. PMID: 41619002 -
bioRxiv
2024 Mar 7:2024.03.04.583390. PMID: 38496520
Solvent & Solubility
DMSO : 25 mg/mL (86.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[1]. Chen Z, 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. [Content Brief]
[2]. Kodama T, et al. Mechanisms underlying the relaxation by A484954, a eukaryotic elongation factor 2 kinase inhibitor, in rat isolated mesenteric artery. J Pharmacol Sci. 2018 May;137(1):86-92. [Content Brief]
[3]. Kameshima S, et al. Eukaryotic elongation factor 2 kinase mediates monocrotaline-induced pulmonary arterial hypertension via reactive oxygen species-dependent vascular remodeling. Am J Physiol Heart Circ Physiol. 2015 May 15;308(10):H1298-305. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4567 mL | 17.2837 mL | 34.5674 mL | 86.4185 mL |
| 5 mM | 0.6913 mL | 3.4567 mL | 6.9135 mL | 17.2837 mL | |
| 10 mM | 0.3457 mL | 1.7284 mL | 3.4567 mL | 8.6418 mL | |
| 15 mM | 0.2304 mL | 1.1522 mL | 2.3045 mL | 5.7612 mL | |
| 20 mM | 0.1728 mL | 0.8642 mL | 1.7284 mL | 4.3209 mL | |
| 25 mM | 0.1383 mL | 0.6913 mL | 1.3827 mL | 3.4567 mL | |
| 30 mM | 0.1152 mL | 0.5761 mL | 1.1522 mL | 2.8806 mL | |
| 40 mM | 0.0864 mL | 0.4321 mL | 0.8642 mL | 2.1605 mL | |
| 50 mM | 0.0691 mL | 0.3457 mL | 0.6913 mL | 1.7284 mL | |
| 60 mM | 0.0576 mL | 0.2881 mL | 0.5761 mL | 1.4403 mL | |
| 80 mM | 0.0432 mL | 0.2160 mL | 0.4321 mL | 1.0802 mL |
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