2. Apoptosis
  3. Bcl-2 Family
  4. (+)-Apogossypol

(+)-Apogossypol  (Synonyms: Apogossypol; NSC736630)

目录号: HY-13408
产品使用指南

摩尔计算器

(+)-Apogossypol 是一种泛 BCL-2 拮抗剂，与 Mcl-1, Bcl-2 和 Bcl-xL 结合， EC50 分别为 2.6，2.8 和 3.69 μM。

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(+)-Apogossypol Chemical Structure

(+)-Apogossypol Chemical Structure

CAS No. : 66389-74-0

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(+)-Apogossypol 相关抗体

Top Publications Citing Use of Products

查看 Bcl-2 Family 亚型特异性产品:

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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

(+)-Apogossypol is a pan-BCL-2 antagonist. (+)-Apogossypol binds to Mcl-1, Bcl-2 and Bcl-xL with EC50s of 2.6, 2.8 and 3.69 µM, respectively.

IC50 & Target[1]

Mcl-1

2.6 μM (EC50)

Bcl-2

2.8 μM (EC50)

Bcl-xL

3.69 μM (EC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HeLa IC50
14.1 μM
Compound: (12b, (-)-apogossypol
Anticancer activity against human HeLa cells after 48 hrs by MTT assay
Anticancer activity against human HeLa cells after 48 hrs by MTT assay
[PMID: 19447525]
HeLa IC50
25.5 μM
Compound: 12a, (+)-apogossypol
Anticancer activity against human HeLa cells after 48 hrs by MTT assay
Anticancer activity against human HeLa cells after 48 hrs by MTT assay
[PMID: 19447525]
NCI-H1299 EC50
3.4 μM
Compound: 2, Apogossypol
Cytotoxicity against human H1299 cells assessed as cell viability after 72 hrs by ATP-LITE assay
Cytotoxicity against human H1299 cells assessed as cell viability after 72 hrs by ATP-LITE assay
[PMID: 19555126]
NCI-H460 EC50
3.5 μM
Compound: 2, Apogossypol
Cytotoxicity against human H460 cells assessed as cell viability after 72 hrs by ATP-LITE assay
Cytotoxicity against human H460 cells assessed as cell viability after 72 hrs by ATP-LITE assay
[PMID: 19555126]
U-87MG ATCC IC50
28.5 μM
Compound: (12b, (-)-apogossypol
Anticancer activity against human U87 cells after 48 hrs by MTT assay
Anticancer activity against human U87 cells after 48 hrs by MTT assay
[PMID: 19447525]
U-87MG ATCC IC50
35.5 μM
Compound: 12a, (+)-apogossypol
Anticancer activity against human U87 cells after 48 hrs by MTT assay
Anticancer activity against human U87 cells after 48 hrs by MTT assay
[PMID: 19447525]
体外研究
(In Vitro)

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[1].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[2].

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

(+)-Apogossypol 相关抗体:
体内研究
(In Vivo)

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)[2].

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

462.54

Formula

C28H32O6
CAS 号
中文名称

變棉子酚；阿朴棉子酚；变棉子酚
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献
Cell Assay
[2]

The cytotoxic effect of (+)-Apogossypol and Gossypol on prostate cancer cell lines is measured by the MTT assay. LNCaP cells are seeded onto sterile 96 well flat bottomed plates and incubated overnight. Then diluted (+)-Apogossypol (1 and 10 μM) and Gossypol are added into each well with gradient concentrations (2-20 μM). For the cell viability test, tumor cells are suspended in a mixed solution of 200 μL complete medium and 0.2 μL DMSO, and wells with 200 μL complete medium are used as blank controls. The plates are incubated at 37°C with 5% CO2 for 72 h. The medium is then removed, and 0.5 μM MTT is added into the wells. After another 4 h, 150 μL DMSO is added into each well. The absorbance is read at 570 nm on a microplate reader. The drug concentration yielding 50% cell inhibition (IC50) is determined. All experiments are performed in triplicate[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
Female athymic nude (nu/nu) mice (4-6 weeks of age, weighing 20-25 g) are used. LNCaP cells (2×106) are injected subcutaneously into each mouse. The tumor volume is measured every two days using a caliper and calculated. When subcutaneous tumor sizes reach 150-200 mm3, these mice are randomly divided into three groups, each group consisting of 10 mice. Next, they are treated with (+)-Apogossypol and Gossypol, respectively, at 20 mg/kg intraperitoneally, q.d. every 7 d for 28 d. The vehicle control group receive the same amount of DMSO as in the treatment groups. The tumor volume is detected every day. The tumor tissues are fixed in 10% formalin solution. The tissues are embedded with paraffin, and the sections are prepared. Samples are stained with hematoxylin and eosin and microscopically examined.

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

(+)-Apogossypol 相关分类

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  • 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:

(+)-Apogossypol66389-74-0Apogossypol NSC736630變棉子酚阿朴棉子酚变棉子酚NSC736630NSC 736630NSC-736630Bcl-2 FamilyInhibitorinhibitorinhibit

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