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General description
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 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-xL-dependent cells, even at a concentration of 5 µM. Preferentially binds Bcl-2 (Ki = 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.
Biochem/physiol Actions
Cell permeable: yes
Product does not compete with ATP.
Reversible: no
Target Ki: 1.3 µM in binding Bcl-2
Packaging
Packaged under inert gas
Other Notes
Real, P.J., et al. 2004. Cancer Res. 64, 7947.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Carcinogenic / Teratogenic (D)
| Quality Segment | 100 |
| assay | ≥90% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | red |
| solubility | DMSO: 5 mg/mL,ethanol: 5 mg/mL |
| shipped in | wet ice |
| storage temp. | −20°C |
| SMILES string | [s]1c2c(nc1Nc4ccc(cc4)OC(=O)C(NC(=O)OC)CCSC)C(=O)c3c(cccc3)C2=O |
| InChI | 1S/C24H21N3O6S2/c1-32-24(31)26-17(11-12-34-2)22(30)33-14-9-7-13(8-10-14)25-23-27-18-19(28)15-5-3-4-6-16(15)20(29)21(18)35-23/h3-10,17H,11-12H2,1-2H3,(H,25,27)(H,26,31) |
| InChI key | SFDSXIZFOOBDMC-UHFFFAOYSA-N |
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