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Beschreibung

A cell-permeable nitrophenylsulfonylbenzamide compound that is shown to bind anti-apoptotic Bcl-2 family members Bcl-2, Bcl-XL, and Bcl-w with high affinity (Ki &le, 1 nM) and serves as a nonpeptidyl alternative to Bad-derived BH3 peptide (Cat. No. 197220) in preventing the binding and inhibition of the pro-apoptotic by the anti-apoptotic Bcl-2 family proteins. ABT-737 is demonstrated to fully reverse the blockage of Myr-Bid-induced cytochrome c release by Bcl-2 in mitochondria preparations from Bcl-2 overexpressing FL5.12 cells and effectively inhibit the growth of numerous cancer cells both in cultures in vitro (IC50 &le,100 nM against H146 and H1963) and in vivo (complete regression of H146 and H1963 in xenograft mice at 100 mg/kg/day, i.p.). Application of ABT-737 is also demonstrated to significantly reduce the disease severity in several murine models of autoimmunity. Also available as a 25 mM solution in DMSO (Cat. No. 197334)., A cell-permeable nitrophenylsulfonylbenzamide compound that is shown to bind anti-apoptotic Bcl-2 family members Bcl-2, Bcl-XL, and Bcl-w with high affinity (Ki &le,1 nM) and serves as a nonpeptidyl alternative to Bad-derived BH3 peptide (Cat. No. 197220) in preventing the binding and inhibition of the pro-apoptotic by the anti-apoptotic Bcl-2 family proteins. ABT-737 is demonstrated to fully reverse the blockage of Myr-Bid-induced cytochrome c release by Bcl-2 in mitochondria preparations from Bcl-2 overexpressing FL5.12 cells and effectively inhibit the growth of numerous cancer cells both in cultures in vitro (IC50 &le,100 nM against H146 and H1963) and in vivo (complete regression of H146 and H1963 in xenograft mice at 100 mg/kg/day, i.p.). Application of ABT-737 is also demonstrated to significantly reduce the disease severity in several murine models of autoimmunity.