耗材描述
(R)-(-)-Gossypol
产品活性:(R)-(-)-Gossypol (AT-101) 是天然产物 Gossypol 的左旋异构体。(R)-(-)-Gossypol (AT-101) 结合到 Bcl-2,Mcl-1 和 Bcl-xL 蛋白,Ki 值分别为 260±30 nM,170±10 nM 和 480±40 nM。
产品来源: https://www.medchemexpress.cn/AT-101.html
研究领域:Apoptosis | Autophagy
作用靶点:Bcl-2 Family | Autophagy
来源:植物 | 锦葵科 | 棉属
结构分类:酚类 | 结构分类
In Vitro: The natural racemic Gossypol has two enantiomers, namely the (R)-(-)-Gossypol (AT-101) and (+)-Gossypol enantiomers. (R)-(-)-Gossypol (AT-101) and (+)-Gossypol binds to Bcl-2 or Bcl-xL with similar binding affinities, AT-101 is more potent than (+)-Gossypol in inhibition of cell growth and induction of apoptosis, possibly due to the influence of serum in the cell culture experiments. 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. AT-101 exhibits greater growth inhibition relative to (±)-Gossypol than (+)-Gossypol in both cell lines tested (P50 of 2-5 μM and a less sensitive group with IC50 clusters around 10 μM. (R)-(-)-Gossypol (AT-101) is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Ki values of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.
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