BAY 87-2243

Biological Activity

BAY 87-2243 is a mitochondrial 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.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. 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.
   Cancer Med
2. 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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