Tirapazamine is an anticancer chemotherapeutic compound currently in clinical trials co-administered with cisplatin or radiation as a potential treatment for several cancers. Tirapazamine inhibits DNA topoisomerase IIα and modulates replication protein A (RPA), inhibiting DNA replication. Tirapazamine also forms DNA damaging free radicals, inducing single- and double-stranded DNA breaks. Additionally, tirapazamine inhibits expression of HIF-1α, potentially through modulation of eukaryotic initiation factor eIF2α phosphorylation. This compound induces apoptosis in neuroblastoma cells, decreasing the mitochondrial membrane potential and levels of glutathione; this effect may be p53-dependent.