vlx600

VLX600 is a small molecule iron chelator and inhibitor of mitochondrial oxidative phosphorylation (OXPHOS), specifically targeting complexes I, II, and IV. It is a lipophilic cation-based triazinoindolyl-hydrazone compound with potential antineoplastic activity. By inhibiting OXPHOS in tumor cells—especially in metabolically compromised microenvironments—VLX600 induces a shift to glycolysis via hypoxia-inducible factor 1-alpha (HIF-1α), but glycolysis alone cannot sustain tumor cell survival under these conditions. This leads to nutrient depletion, decreased energy production, induction of autophagy and mitophagy (autophagy-dependent cell death), and ultimately tumor cell death. VLX600 has demonstrated selective cytotoxicity against both proliferating and quiescent cancer cells—including glioblastoma stem-like cells—and has been evaluated in phase I clinical trials for advanced solid tumors[2][3][4][5][6]. The drug’s mechanism involves both iron chelation and disruption of mitochondrial function.

Other names

6-methyl-3-(2-(1-(pyridin-2-yl)ethylidene)hydrazinyl)-5H-[1,2,4]triazino[5,6-b]indole