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Description

A cell-permeable naphthoquinone compound that selectively induces apoptosis of Bcl-2-overexpressing cells (<300 nM in MDA-MB435B breast cancer cells) with little effect on a variety of primary cells, and Bcl-xL-dependent cells, even at a concentration of 5 µ,M. Preferentially binds Bcl-2 (Ki = 1.3 µ,M) and disrupts its interaction with Bid BH3, thereby blocking the anti-apoptotic activity of Bcl-2. Shown to induce the release of cytochrome c from mitochondria and activate caspase-9., A cell-permeable molecule that targets the BH3.domain interaction and selectively induces apoptosis in Bcl-2-overexpressing cells (<300 nM in MDA-MB435B breast cancer cells). Exhibits little effect on a variety of primary cells and Bcl-xL-dependent cells, even at a concentrations as high as 5 µ,M. Inhibits the binding of Bid BH3 to Bcl-2 thereby blocking the anti-apoptotic activity of Bcl-2.