(+)-Apogossypol is a pan-BCL-2 antagonist that binds to Mcl-1, Bcl-2 and Bcl-xL with EC50 of 2.6, 2.8 and 3.69 μM, respectively.
In agreement with NMR binding and fluorescence polarization assays (FPAs) data, (+)-Apogossypol displays potent binding affinity to Bcl-xL with K d values of 1.7 μM.
Due to its modified structure, (+)-Apogossypol is expected to exhibit lower toxicity while maintaining the significant anti-growth and anti-tumor activities in vitro, similar to those of Gossypol.
| Mcl-1 < span> 2.6 μM (EC 50 ) | Bcl-2 2.8 μM (EC 50 ) | Bcl-xL 3.69 μM (EC 50 ) |
