A 484954 |
| Katalog-Nr.GC12739 |
A 484954 ist ein hochselektiver Hemmer des eukaryotischen Elongationsfaktors 2 (eEF2) mit einem IC50-Wert von 280 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 142557-61-7
Sample solution is provided at 25 µL, 10mM.
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A 484954 is a selective inhibitor of eEF2K with IC50 value of 0.28 μM [1].
Eukaryotic elongation factor-2 kinase (eEF2K) is a calcium/calmodulin-dependent protein kinase and regulates protein synthesis. It phosphorylates eEF2 and inhibits the activity of eEF2 [1].
A 484954 is a selective eEF2K inhibitor. A 484954 inhibited eEF2K and the phosphorylation of eEF2. While, it didn’t inhibit cancer cell growth. In enzymatic assay, the IC50 value of A-484954 was increased in an ATP-dependent way but not affected by the concentrations of calmodulin. In H1299 cells, A 484954 inhibited the phosphorylation of eEF2 but didn’t affect the protein level of eEF2. In PC3 cells, A 484954 (10 μM) inhibited peEF2 by 50% and the inhibition reached the maximum level at 100 μM. While A 484954 didn’t inhibit cell proliferation. In PC3 cells, NH125 induced eEF2 phosphorylation, while A 484954 had little effect on peEF2 induced by NH125 [1].
Reference:
[1]. Chen Z, Gopalakrishnan SM, Bui MH, 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, 286(51): 43951-43958.
| Cas No. | 142557-61-7 | SDF | |
| Chemical Name | 7-amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-6-carboxamide | ||
| Canonical SMILES | O=C(N(CC)C1=O)N(C2=NC(N)=C(C(N)=O)C=C21)C3CC3 | ||
| Formula | C13H15N5O3 | M.Wt | 289.29 |
| Löslichkeit | <2.89mg/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 | 3.4567 mL | 17.2837 mL | 34.5674 mL |
| 5 mM | 0.6913 mL | 3.4567 mL | 6.9135 mL |
| 10 mM | 0.3457 mL | 1.7284 mL | 3.4567 mL |
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