Bcl-2 Inhibitor II, YC137

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-x_L-dependent cells, even at a concentrations as high as 5 µM. Inhibits the binding of Bid BH3 to Bcl-2 thereby blocking the anti-apoptotic activity of Bcl-2.

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-x_L-dependent cells, even at a concentration of 5 µM. Preferentially binds Bcl-2 (K_i = 1.3 µM) 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.

Cell permeable: yes

Product does not compete with ATP.

Reversible: no

Target K_i: 1.3 µM in binding Bcl-2

Packaged under inert gas

Real, P.J., et al. 2004. Cancer Res. 64, 7947.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Carcinogenic / Teratogenic (D)