(S)-Gossypol (acetic acid)

(S)-Gossypol is the isomer of a natural product Gossypol. (S)-Gossypol binds to the BH3-binding groove of Bcl-xL and Bcl-2 proteins with high affinity.

Signaling Pathways >> Apoptosis >> Bcl-2 Family

Research Areas >> Cancer

Bcl-2

Bcl-xL

The natural racemic Gossypol has two enantiomers, namely the (-)-Gossypol and (S)-Gossypol ((+)-Gossypol) enantiomers. (+)-Gossypol and (-)-Gossypol binds to Bcl-2 or Bcl-xL with similar binding affinities. (-)-Gossypol is more potent than (+)-Gossypol in inhibition of cell growth and induction of apoptosis. The racemic form and each of the enantiomers of Gossypol are tested against UM-SCC-6 and UM-SCC-14A in 6-day MTT assays. (-)-Gossypol exhibits greater growth inhibition relative to (±)-Gossypol than (+)-Gossypol in both cell lines tested (P<0.001). An intermediate growth inhibitory effect is observed with (±)-Gossypol but this effect is only observed at the higher dose of Gossypol (10 μM, P<0.0001)[1].

Two representative UM-SCC cell lines, UM-SCC-6 and UM-SCC-14A, are continuously exposed to 0 (vehicle control), 5 or 10 μM (±)-Gossypol, (-)-Gossypol or (S)-Gossypol ((+)-Gossypol) in a 6-day MTT cell survival assay[1].

[1]. Oliver CL, et al. In vitro effects of the BH3 mimetic, (-)-Gossypol, on head and neck squamous cell carcinoma cells. Clin Cancer Res. 2004 Nov 15;10(22):7757-63.

Venetoclax (ABT-199) | ABT-263 | S63845 | ABT-737 | Obatoclax Mesylate | A-1210477 | A-1155463 | WEHI-539 hydrochloride | A-1331852 | Bax inhibitor peptide V5 | FX 1 | Gambogic Acid | TW-37 | UMI-77 | Acetate gossypol