Bcl-2 Inhibitor II, YC137 is 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. Bcl-2 Inhibitor II, YC137 preferentially binds Bcl-2 (Ki = 1.3 μM) and disrupts its interaction with Bid BH3, thereby blocking the anti-apoptotic activity of Bcl-2. This has shown to induce the release of cytochrome c from mitochondria as well as activate caspase-9.
Real, P.J., et al. 2004. Cancer Res. 64, 7947.
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