Aaptamine Inhibitor

Solid. Powder

98.00%

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

228.25

<1mg/ml refers to the product slightly soluble or insoluble

C13H12N2O2

COc1cc2ccnc(C=CN3)c2c3c1OC

85547-22-4

p53
TNF-alpha
c-Myc

All Aaptamines were found to be equally effective in both cell lines, excluding cross-resistance between Aaptamines and cisplatIn 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]

Apoptosis; p53; Cell Cycle/Checkpoint