Exhaustive explorations of chemical probe 7 led to several revelations such as (i) compound 7 increasedapoptosis/necrosis-related gene expression, whereas decreased M phase/kinetochore/spindle-relatedgene expression as well as CENPs protein expression in Pt3R cells;(ii) dual inhibitor 7 induced cell cycle arrest at theM phase; (iii) compound 7 suppressed reactive oxygenspecies (ROS) catabolism pathway, causing the death of TMZ-resistantGBM cells; and (iv) compound 7 elicited substantial in vivo anti-GBM efficacy in experimental mice xenograftedwith TMZ-resistant Pt3R cells. The gene discussed is CENPS; the disease is glioblastoma.