Chemical Name: 1-Cyclopropyl-4-[4-[[5-methyl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]-1H-pyrazol-1-yl]methyl]-2-pyridinyl]piperazine
Biological ActivityMitochondrial complex I inhibitor. Exhibits no effect on mitochondrial complex III. Induces mitochondrial permeability transition pore (mPTP) opening, stimulates autophagosome formation and mitophagy, and increases ROS levels. Activates necroptotic and ferroptotic cell death. Also inhibits hypoxia-induced gene activation. Induces cell death in melanoma cell lines in vitro and exhibits antitumor activity in a mouse NSCLC xenograft model in vivo.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I.
Ellinghaus P, Heisler I, Unterschemmann K et al.
Mitochondrial complex I inhibition triggers a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis in melanoma cells.
Basit et al.
Cell Death Dis., 2017;8:e2716
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