Deoxyvasicinone
Deoxyvasicinone derivatives can be considered as promising lead molecules for the development of more potent inhibitors of NEDD8-activating enzyme.
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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Methods. 2015 Jan;71:71-6.
Discovery of deoxyvasicinone derivatives as inhibitors of NEDD8-activating enzyme.[Pubmed:
25196325]
NEDD8-activating enzyme (NAE) controls the specific degradation of proteins regulated by cullin-RING ubiquitin E3 ligases, and has been considered as an attractive molecular target for the development of drugs against cancer.
METHODS AND RESULTS:
A pharmacophore model constructed from a training set of Deoxyvasicinone derivatives was used to screen 376 compounds from an analogue database. From the initial screening, the valine-linked Deoxyvasicinone derivative 9 and the N-isopropyl-linked Deoxyvasicinone derivative 10 emerged as the top scoring candidates. Compounds 9 and 10 showed micromolar potencies in both cell-free and cell-based systems, with selectivity for NAE over the related enzymes SAE and UAE. Molecular modelling analysis suggested that 9 and 10 may inhibit NAE by blocking the ATP-binding domain.
CONCLUSIONS:
Thus, these Deoxyvasicinone derivatives could be considered as promising lead molecules for the development of more potent inhibitors of NAE.
