2,9-Dimethoxy-11,12-dihydrodibenzo[c,g][1,2]-diazocine 5,6-dioxide (A) and 5,5′-Dimethoxy-2,2′-dinitrosobenzyl (B) Green solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. Contains mixture of two tautomers (A and B). A potent, cell-permeable, Bcl-2 inhibitor that competes with Bak BH3 peptide for binding to Bcl-2 and Bcl-xL in vitro (IC50 = 10 µM and 7 µM, respectively). Reduces cell viability and growth in the HL-60 cell line with high Bcl-2 expression (IC50 = 4 µM). Also induces apoptosis in a dose-dependent manner in cancer cells exhibiting high Bcl-2 expression with little effect on cancer cells with low Bcl-2 expression. Purity: ≥97% by TLC. Ref.: Enyedy, I.J., et al. 2001. J. Med. Chem. 44, 4313. |
