Being a modem technique with the ability of studying, discovering, probing and analyzing the expression of thousands genes, even the whole genome in the only one experiment, microarray proved to be a powerful tool for cancer research especially at molecular level. Employing the potential anticancer compound 1-(5,7dimetoxy-2,2-dimetyl-2H-cromen-8-yl)-but-2-en-l-on (2B2D) and LU-l human lung cancer cells as studied objects, the authors successfully hybridized the cy3/5 incorporated cDNA with Phalanx HOV5 microarray. The results showed that 742 genes got an effect with equal or over two folds changed by 2B2D treatment on LU-l cells. Among of those, 386 genes were up-regulated while 356 were down-regulated. The Nuclear factor (erythroidderived 2, regulatory factor X domain containing 1, fibroblast growth factor receptor 3 (achondroplasia, thanatophoric dwarfism) and E2F transcription factor 8 genes were the most stimulated by 2B2D. In contrast, Solute carrier family 7 (cationic amino acid transporter, system) member 11, kelch-like 24 and Hypothetical LOC344887 were the most down in expression.