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Aaptamine

Catalog No. TN1354   CAS 85547-22-4

Aaptamine functions as a proteasome inhibitor, it activates p21 promoter in a p53-independent manner.

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Aaptamine Chemical Structure
Aaptamine, CAS 85547-22-4
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Aaptamine functions as a proteasome inhibitor, it activates p21 promoter in a p53-independent manner.
In vitro All Aaptamines were found to be equally effective in both cell lines, excluding cross-resistance between Aaptamines and cisplatin in vitro. At the inhibitory concentration (IC50), Aaptamine exerted an antiproliferative effect, whereas demethyloxyAaptamine and isoAaptamine were strong inducers of apoptosis. We analyzed the changes in the proteome of NT2-R cells treated with these compounds. 16-22 proteins were found to be significantly altered, of which several were validated by Western blotting and two-dimensional Western blotting analysis. Changes in the proteome pattern frequently resulted from post-transcriptional protein modifications, i.e. phosphorylation or hypusination in the case of eIF5A. Although the lists of altered proteins were heterogeneous and compound-specific, gene ontology analyses identified rather similar profiles regarding the affected molecular functions. Ingenuity pathway analysis by IPA put the following factors in a central position of the hypothetical networks: myc and p53 for Aaptamine; tumor necrosis factor (TNF) for demethyloxyAaptamine; and all three, myc, p53, and TNF for isoAaptamine[1]
Molecular Weight 228.25
Formula C13H12N2O2
CAS No. 85547-22-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Activity of aaptamine and two derivatives, demethyloxyaaptamine and isoaaptamine, in cisplatin-resistant germ cell cancer.J Proteomics. 2014 Jan 16;96:223-39.

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Keywords

Aaptamine 85547-22-4 Apoptosis Cell Cycle/Checkpoint TNF c-Myc p53 inhibitor inhibit

 

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