(+)-Apogossypol is apan-BCL-2antagonist. (+)-Apogossypol binds toMcl-1,Bcl-2andBcl-xLwithEC₅₀s 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_dvalues of 1.7 μM^[1].To investigate the inhibitory effects of (+)-Apogossypol and Gossypol on LNCaP cell survival, the MTT assay is performed. The results demonstrate that (+)-Apogossypol inhibits the proliferation of LNCaP cells in a time- and dose-dependent manner, in a similar way with Gossypol. The concentration for 50% inhibition (IC₅₀) on LNCaP cells within ~72 h is 9.57 μM, while the IC₅₀of Gossypol on LNCaP cells is 10.35 μM^[2].

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. The anti-cancer effect of (+)-Apogossypol is evaluated in mice bearing subcutaneous LNCaP cell xenografts. The tumor growth is monitored and measured by a caliper and balance. The survival rate of the mice is notably improved by (+)-Apogossypol. Of note, the tumor sizes are also markedly decreased by (+)-Apogossypol treatment (P<0.01)^[2].

462.54

C₂₈H₃₂O₆

66389-74-0

變棉子酚；阿朴棉子酚；变棉子酚

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