For research use only. Not Intended for Therapeutic Use!
|IC50:||18.1μM (Bcl-2), 22.9μM (Bcl-xL)|
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|Product-Name:||(S)-Gossypol acetic acid|
(S)-Gossypol acetic acid is a inhibitor of Bcl-2, potently induce cell death in Jurkat cells overexpressing Bcl-2 (IC50, 18.1μM) or Bcl-xL (IC50, 22.9μM).
IC50 Value: 18.1μM (Bcl-2), 22.9μM (Bcl-xL)
in vitro: Gossypol-acetic acid significantly inhibited the proliferation of RAW264.7 cells in a dose-dependent manner, and caused obvious cell apoptosis and a loss of ΔΨm in RAW264.7 cells. Gossypol-acetic acid-induced cell apoptosis was markedly inhibited by caspase inhibitors . gossypol acetate resulted in a dose- and time-dependent inhibition of multiple myeloma cell proliferation, with an IC50 value to both U266 and Wus1 cells at 2.4, 2.2 μM at 48 h after treatment. Gossypol acetate effectively induced the apoptosis of multiple myeloma cells. Colorimetric assays showed activation of both caspase-3 and caspase-9. Bcl-2 and Bcl-xl expression was decreased by 86.5% and 35.9%, respectively, after treatment with gossypol acetate at 25 μM for 24 h . Gossypol-acetic acid (5-40 μM) inhibited the growth of MEC-1 cells in a dose- and time-dependent manner. Gossypol-acetic acid inhibits the proliferation of MEC-1, and DSB maybe one of the mechanisms of inhibitory effect of Gossypol-acetic acid on the growth of tumor cells .
in vivo: A growth inhibition (T/C) of 30.9% (gossypol acetate 40 mg/kg) was obtained in Balb/C mice bearing Wus1 cells. In addition, there was no body weight loss for the treated group in comparison with the vehicle mice . Male rats were treated with gossypol acetic acid, GSH-Px specific activity increased in gossypol acetic acid group. gossypol acetic acid induce significant increases in the hepatic NEFA with remarkable decrease in the total saturated fatty acids with a significant increase of PUFA . Gossypol-acetic acid has selective action on the sperm membrane of the rats, it inhibited sperm Ca2+ influx in a dose-dependent manner, and exerts no effect on the high K+ induced contraction of smooth muscle of isolated rat .
. Deng, S., et al., Gossypol acetic acid induces apoptosis in RAW264.7 cells via a caspase-dependent mitochondrial signaling pathway. J Vet Sci, 2013. 14(3): p. 281-9.
. Lin, J., et al., Induction of apoptosis and antitumor effects of a small molecule inhibitor of Bcl-2 and Bcl-xl, gossypol acetate, in multiple myeloma in vitro and in vivo. Oncol Rep, 2013. 30(2): p. 731-8.
. Guo, Z., et al., [Gossypol acetic acid induces DNA double-strand breaks in human mucoepidermoid carcinoma cell MEC-1]. Sheng Li Xue Bao, 2011. 63(2): p. 164-70.
. El-Sharaky, A.S., et al., Mutual anti-oxidative effect of gossypol acetic acid and gossypol-iron complex on hepatic lipid peroxidation in male rats. Food Chem Toxicol, 2009. 47(11): p. 2735-41.
. Wu, T., et al., [Effects of gossypol acetic acid on human ejaculated sperm Ca2+ influx and rat vas deferens contraction action]. Zhongguo Yi Xue Ke Xue Yuan Xue Bao, 1996. 18(5): p. 375-9.