BXI-72 (NSC334072, Hoechst 33342) is a potent, selective small molecule Bcl-XL inhibitor that targets the BH3 domain of Bcl-XL (Kd=0.9 nM).
BXI-72 displays very low binding affinities with Bcl2 (Ki=283 nM), Mcl-1, Bcl-w and Bfl-1/A1 (Ki>1500 nM).
BXI-72 potently suppresses lung cancer cell growth (H1299=0.49 uM, A549 IC50=0.68 uM), displays relatively selective cytotoxicity against lung cancer cells compared to normal human bronchial epithelial cells.
BXI-72 causes disruption of Bcl-XL/Bak or Bcl-XL/Bax interaction, oligomerization of Bak, and cytochrome c release from mitochondria in cells.
BXI-72 exhibits more potent efficacy against human lung cancer than ABT-737 but less degree in platelet reduction in vivo.
BXI-72 (NSC334072, Hoechst 33342) is a marker dye in Hoechst series for live nuclear marker dye.
