Apogossypol

Research use only, not for human use.

Apogossypol (NSC 736630) is a Bcl-2 family antagonist that binds to Bcl-XL, Bcl-2 and Bcl-xL with IC50 of 2.6, 2.8 and 3.69 uM, respectively.

Apogossypol (NSC 736630) is a Bcl-2 family antagonist that binds to Bcl-XL, Bcl-2 and Bcl-xL with IC50 of 2.6, 2.8 and 3.69 uM, respectively; induces apoptosis of tumor cell lines, inhibits the growth and proliferation of prostate cancer cells by downregulating Bcl?2 protein expression and activating caspase?3 and ?8; displays superior activity to gossypol in terms of reducing splenomegaly and reducing B-cell counts in spleens of Bcl-2-transgenic mice.

In agreement with NMR binding and fluorescence polarization assays (FPAs) data, (+)-Apogossypol displays potent binding affinity to Bcl-xL with Kd values of 1.7 μM.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 IC50 of Gossypol on LNCaP cells is 10.35 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. 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).

+)-Apogossypol | NSC 736630

Angiogenesis

Bcl-2

Bcl-2

Cancer

——

66389-74-0

462.53

C28H30O6

>98% (HPLC)

10 mM in DMSO

CC1=CC2=C(C(=C(C=C2C(=C1C3=C(C4=CC(=C(C(=C4C=C3C)C(C)C)O)O)O)O)O)O)C(C)C

[2,2'-Binaphthalene]-1,1',6,6',7,7'-hexol, 3,3'-dimethyl-5,5'-bis(1-methylethyl)-, (2S)-

(-20℃)

With Ice Pack

≥ 2 years