Abstract: OBJECTIVE To explore the effect and mechanism of benzyl isothiocyanate on the invasion inhibition and apoptosis induce of human glioma cancer U87MG cell lines. METHODS MTS assay was employed to determine the effect of benzyl isothiocyanate on the proliferation of tumor cells. After treatment with 2 and 5 μmol·L^-1 benzyl isothiocyanate, Transwell assay, adhesion assay and scratch assay were employed to evaluate the potential of invasive, adhesion and migration in U87MG human glioma cells. Real-time-PCR and western blot assay was employed to evaluate the mRNA and protein expression levels of MMP-2, MMP-9, CD44, Survivin, Bcl-2, caspase-3, caspase-8, Net1, RohA and p-AKT. Report gene assay was employed to evaluate the transcriptional activity of NF-κB, ELISA assay was employed to detect the level of 8-OH-dG, flow cytometry assay was employed to evaluate the apoptosis rate with 10 and 20 μmol·L^-1 benzyl isothiocyanate treatment. RESULTS benzyl isothiocyanate significantly inhibited the proliferation of U87MG. With 2 and 5 μmol·L^-1 benzyl isothiocyanate, the invasion of U87MG cells was inhibited, the expression of MMP-2, MMP-9, CD44, Survivin, Bcl-2, NET1, RhoA, p-AKT and the transcriptional activity of NF-κB was down regulated, as well as an increase in activity of caspase-3, caspase-8 and 8-OH-dG level. Apoptosis rate was improved with 10 and 20 μmol·L^-1 benzyl isothiocyanate treatment compared with 0 μmol·L^-1 group. CONCLUSION Benzyl isothiocyanate can significantly inhibit the invasion and induce the apoptosis of human glioma U87MG cell lines via regulation of metastasis and apoptosis-related genes, which may be related to AKT/NF-κB pathways.