A 484954EEF2K Inhibitor CAS# 142557-61-7 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 142557-61-7 | SDF | Download SDF |
| PubChem ID | 14998470 | Appearance | Powder |
| Formula | C13H15N5O3 | M.Wt | 289.29 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 20 mg/mL (69.13 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) | ||
| Chemical Name | 7-amino-1-cyclopropyl-3-ethyl-2,4-dioxopyrido[2,3-d]pyrimidine-6-carboxamide | ||
| SMILES | CCN1C(=O)C2=CC(=C(N=C2N(C1=O)C3CC3)N)C(=O)N | ||
| Standard InChIKey | HWODCHXORCTEGU-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C13H15N5O3/c1-2-17-12(20)8-5-7(10(15)19)9(14)16-11(8)18(13(17)21)6-3-4-6/h5-6H,2-4H2,1H3,(H2,14,16)(H2,15,19) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Inhibitor of eukaryotic elongation factor-2 (eEF-2) kinase (IC50 = 0.28 μM in enzymatic assay). Reduces eEF-2 phosphorylation with little effect on cancer cell growth. |
A 484954 Dilution Calculator
A 484954 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.4567 mL | 17.2837 mL | 34.5674 mL | 69.1348 mL | 86.4185 mL |
| 5 mM | 0.6913 mL | 3.4567 mL | 6.9135 mL | 13.827 mL | 17.2837 mL |
| 10 mM | 0.3457 mL | 1.7284 mL | 3.4567 mL | 6.9135 mL | 8.6418 mL |
| 50 mM | 0.0691 mL | 0.3457 mL | 0.6913 mL | 1.3827 mL | 1.7284 mL |
| 100 mM | 0.0346 mL | 0.1728 mL | 0.3457 mL | 0.6913 mL | 0.8642 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.[Pubmed:22020937]
J Biol Chem. 2011 Dec 23;286(51):43951-8.
Eukaryotic elongation factor-2 kinase (eEF2K) relays growth and stress signals to protein synthesis through phosphorylation and inactivation of eukaryotic elongation factor 2 (eEF2). 1-Benzyl-3-cetyl-2-methylimidazolium iodide (NH125) is a widely accepted inhibitor of mammalian eEF2K and an efficacious anti-proliferation agent against different cancer cells. It implied that eEF2K could be an efficacious anticancer target. However, eEF2K siRNA was ineffective against cancer cells including those sensitive to NH125. To test if pharmacological intervention differs from siRNA interference, we identified a highly selective small molecule eEF2K inhibitor A-484954. Like siRNA, A-484954 had little effect on cancer cell growth. We carefully examined the effect of NH125 and A-484954 on phosphorylation of eEF2, the known cellular substrate of eEF2K. Surprisingly, NH125 increased eEF2 phosphorylation, whereas A-484954 inhibited the phosphorylation as expected for an eEF2K inhibitor. Both A-484954 and eEF2K siRNA inhibited eEF2K and reduced eEF2 phosphorylation with little effect on cancer cell growth. These data demonstrated clearly that the anticancer activity of NH125 was more correlated with induction of eEF2 phosphorylation than inhibition of eEF2K. Actually, induction of eEF2 phosphorylation was reported to correlate with inhibition of cancer cell growth. We compared several known inducers of eEF2 phosphorylation including AMPK activators and an mTOR inhibitor. Interestingly, stronger induction of eEF2 phosphorylation correlated with more effective growth inhibition. We also explored signal transduction pathways leading to NH125-induced eEF2 phosphorylation. Preliminary data suggested that NH125-induced eEF2 phosphorylation was likely mediated through multiple pathways. These observations identified an opportunity for a new multipathway approach to anticancer therapies.
