Using a strategy based on high-throughput chemical screening (HTS) and affinity chromatography, we identified a small molecule NQO1 and GSTP1 dual inhibitor, MNPC, that suppressed the proliferation and stimulated apoptosis in a highly passaged cell line and primary GBM cells bearing the EGFRvIII mutation. The gene discussed is NQO1; the disease is glioblastoma.