Bcl-2-IN-8

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Bcl-2-IN-8 

Bcl-2-IN-8 是一种有效的抗癌剂。Bcl-2-IN-8 对药物敏感和耐药的癌细胞均显示抗增殖活性。Bcl-2-IN-8 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 G1 期。Bcl-2-IN-8 以剂量依赖性方式抑制细胞迁移。Bcl-2-IN-8 具有三阴乳腺癌的研究潜力。

Bcl-2-IN-8

Bcl-2-IN-8 Chemical Structure

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生物活性

Bcl-2-IN-8 is a potent anticancer agent. Bcl-2-IN-8 shows anti-proliferative activity against both drug-sensitive and drug-resistant cancer cells. Bcl-2-IN-8 induce apoptosis and cell cycle arrest at G1 phase. Bcl-2-IN-8 inhibits cell migration in a dose-dependent manner. Bcl-2-IN-8 has the potential for the research of triple negrative breast cancer[1].

IC50 & Target[1]

Bax

 

Bcl-2

 

体外研究
(In Vitro)

Bcl-2-IN-8 (compound 4m) (48 h) shows selective cytotoxicity against MDA-MB-231, MCF-7/ADR, MCF-10A cells with IC50s of 0.51, 0.38, 3.56 µM, respectively[1].
Bcl-2-IN-8 (0-8 µM; 24, 48, 72 h) inhibits cell proliferation in a dose-time dependently[1].
Bcl-2-IN-8 (0-2 µM; 24 h) induces cell cycle arrest at G1 phase in MDA-MB-231 cells[1].
Bcl-2-IN-8 (0-2 µM; 24 h) induces apoptosis in MDA-MB-231 cells[1].
Bcl-2-IN-8 (0-3 µM; 24 h) up-regulates the expression of Bax, cytochrome c and down-regulates Bcl-2, P53 protein in a concentration dependently in MDA-MB-231 cells[1].
Bcl-2-IN-8 (0-3 µM; 24 h) decreases the ΔΨm and induces ROS (reactive oxygen species) generation by activating the p38MAPK-Akt signaling pathway in MDA-MB-231 cells[1].
Bcl-2-IN-8 (0-2 µM; 24 h) increases intracellular Ca2+ concentration from 9.9 treated with DMSO to 37.4 treated at 2 µM in MDA-MB-231 cells[1].
Bcl-2-IN-8 (0-3 µM; 24 h) significantly inhibits migration in a dose-dependent manner in MDA-MB-231 cells[1].
Bcl-2-IN-8 (0-3 µM; 24 h) increases the expression levels of Smad 7 but decreases the expression levels of p-Smad 3 in MDA-MB-231 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1].

Cell Line: MB-231, MCF-7, MCF-7/adriamycin (adriamycin-resistant MCF-7 cell line) cells
Concentration:
Incubation Time: 48 h
Result: Showed potent inhibitory activities on MDA-MB-231, MCF-7, MCF-7/ADR (adriamycin) cells with IC50s of 0.51, 2.01, 0.38 µM, respectively.

Cell Proliferation Assay[1].

Cell Line: MDA-MB-231 cells
Concentration: 0-8 µM
Incubation Time: 24, 48, 72 h
Result: Inhibited cell proliferation in a dose-time dependently.

Cell Cycle Analysis[1].

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 1, 2 µM
Incubation Time: 24 h
Result: Arrested the cell-cycle at the G1 phase and the percentage of cells in the G1 phase from 54.8 to 74.6%.

Western Blot Analysis[1].

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 1, 2, 3 µM
Incubation Time: 24 h
Result: Decreased the expression of cyclin D1, CDK4 and CDK6 protein, but did not influence the expression of c-myc proteins.

Apoptosis Analysis[1].

Cell Line: MDA-MB-231 cells
Concentration: 0, 0.5, 1, 2 µM
Incubation Time: 24 h
Result: The total percentage of early and late apoptosis increased to 10.2%, 17.6%, 56.4% with the concentration of 0.5 µM, 1 µM, 2 µM.

体内研究
(In Vivo)

Bcl-2-IN-8 shows metabolic stability with CL50 value of 14.1 mL/min/mg and remaining (T=100 min) of 18.5% in rats[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

572.73

Formula

C36H44O6

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.

参考文献
  • [1]. Liang JJ, et al. Synthesis and structure-activity relationship study of a potent MHO7 analogue as potential anti-triple negative breast cancer agent. Eur J Med Chem. 2022 Jun 5;236:114313.

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