2. Apoptosis Autophagy
  3. Bcl-2 Family Autophagy
  4. (R)-(-)-Gossypol

(R)-(-)-Gossypol  (Synonyms: AT-101; R-(-)-gossypol acetic acid)

目录号: HY-15464 纯度: 98.82%
COA 产品使用指南

摩尔计算器

(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。

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(R)-(-)-Gossypol Chemical Structure

(R)-(-)-Gossypol Chemical Structure

CAS No. : 90141-22-3

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规格 价格 是否有货 数量
5 mg ￥2300
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10 mg ￥3700
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100 mg   询价  

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Other Forms of (R)-(-)-Gossypol:

(R)-(-)-Gossypol 相关抗体

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

(R)-(-)-Gossypol (AT-101) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.

IC50 & Target[2]

Mcl-1

170 nM (Ki)

Bcl-2

260 nM (Ki)

Bcl-xL

480 nM (Ki)

Autophagy

 

体外研究
(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 (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). (R)-(-)-Gossypol (AT-101) binds to the BH3-binding groove of Bcl-xL and Bcl-2 proteins with fairly high affinity, has potent activity against head and neck squamous cell carcinomas (HNSCC) cell lines in vitro. Furthermore, it induces apoptosis with high efficiency in HNSCC tumor cells that express functional p53 and that also kills tumor cells with mutant p53 by a different mechanism. AT-101 doses required to inhibit the growth of human fibroblast cell lines by 50% were 2- to 10-fold higher than for HNSCC cell lines. To inhibit human oral keratinocyte growth by 50%, (R)-(-)-Gossypol (AT-101) concentrations are 2-to 3-fold higher than for HNSCC cell lines. (R)-(-)-Gossypol (AT-101) causes dose-dependent inhibition of cell growth in ten UM-SCC cell lines over a range from 0.5 to 10 μM in a 6-day MTT assay. The relative sensitivity of the cell lines vary from a very sensitive group with an IC50 of 2-5 μM and a less sensitive group with IC50 clusters around 10 μM[1]. (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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

(R)-(-)-Gossypol 相关抗体:
Clinical Trial
分子量

518.55

Formula

C30H30O8
CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

(R)-(-)-棉子酚
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 200 mg/mL (385.69 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9285 mL 9.6423 mL 19.2845 mL
5 mM 0.3857 mL 1.9285 mL 3.8569 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Cell Assay
[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, (R)-(-)-Gossypol or (+)-Gossypol in a 6-day MTT cell survival assay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

(R)-(-)-Gossypol 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9285 mL 9.6423 mL 19.2845 mL 48.2114 mL
5 mM 0.3857 mL 1.9285 mL 3.8569 mL 9.6423 mL
10 mM 0.1928 mL 0.9642 mL 1.9285 mL 4.8211 mL
15 mM 0.1286 mL 0.6428 mL 1.2856 mL 3.2141 mL
20 mM 0.0964 mL 0.4821 mL 0.9642 mL 2.4106 mL
25 mM 0.0771 mL 0.3857 mL 0.7714 mL 1.9285 mL
30 mM 0.0643 mL 0.3214 mL 0.6428 mL 1.6070 mL
40 mM 0.0482 mL 0.2411 mL 0.4821 mL 1.2053 mL
50 mM 0.0386 mL 0.1928 mL 0.3857 mL 0.9642 mL
60 mM 0.0321 mL 0.1607 mL 0.3214 mL 0.8035 mL
80 mM 0.0241 mL 0.1205 mL 0.2411 mL 0.6026 mL
100 mM 0.0193 mL 0.0964 mL 0.1928 mL 0.4821 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(R)-(-)-Gossypol90141-22-3AT-101 R-(-)-gossypol acetic acid(R)-(-)-棉子酚AT101AT 101Bcl-2 FamilyAutophagyInhibitorinhibitorinhibit

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