GL0388

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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。

GL0388 

GL0388 是一种 Bax 激活剂，可导致 Bax 插入线粒体膜。GL0388 对多种癌细胞具有抗增殖活性，IC50 值为 0.299-1.57 μM。GL0388 激活 Bax 并诱导 Bax 介导的细胞凋亡。GL0388 在体内抑制乳腺癌异种移植肿瘤的生长。

GL0388

GL0388 Chemical Structure

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生物活性

GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo[1].

IC50 & Target[1]

Bax

 

体外研究
(In Vitro)

GL0388 (0.1-10 μM; 72 h) inhibits the cell proliferation of MDA-MB-231 and MCF-7 breast cancer cell lines, with IC50s of 0.96 μM and 0.52 μM, respectively[1].
GL0388 (0.01-100 μM) inhibits the cell proliferation in 60 human tumor cell lines, with GI550s of 0.299-1.57 μM[1].
GL0388 (1-10 μM; 48 h) significantly upregulates the cleaved PARP-1 and cleaved caspase 3 in MDA-MB-231 cells[1].
GL0388 (0.1-1 μM; 24 h) inhibits the colony formation and invasion of breast cancer cells[1].
GL0388 (1-10 μM; 24 h) promotes Bax insertion into mitochondrial membranes of MDA-MB-231 cells in a dose-dependent manner. GL0388 increases cytochrome c in the cytosolic fraction of 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 Proliferation Assay[1]

Cell Line: MCF-7, MDA-MB-231 cells
Concentration: 0.1, 0.33, 1, 3.3, 10 μM
Incubation Time: 72 hours
Result: Inhibited the growth of MCF-7, MDA-MB-231 cells, with IC50s of 0.52 μM and 0.96 μM, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 1, 5, 10 μM
Incubation Time: 48 hours
Result: Significantly led to the upregulation of cleaved PARP-1 and cleaved caspase 3.

体内研究
(In Vivo)

GL0388 (10-20 mg/kg for i.p.; 15 mg/kg for i.t.; once daily for 10 days) dose-dependently suppresses the growth of MDA-MB-231 tumors in mice[1].

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

Animal Model: Female nude mice were injected MDA-MB-231 cells[1]
Dosage: 10-20 mg/kg for i.p.; 15 mg/kg for i.t.
Administration: I.p and i.t. once daily for 10 days
Result: Significantly inhibited tumor growth at a dose of 15 mg/kg every other day.
I.T. administration for 10 consecutive days, with an inhibition rate of 55%, comparable to the I.P. efficacy at the dose of daily 20 mg/kg.

分子量

332.37

Formula

C21H17FN2O
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]. Liu G, et, al. Further lead optimization on Bax activators: Design, synthesis and pharmacological evaluation of 2-fluoro-fluorene derivatives for the treatment of breast cancer. Eur J Med Chem. 2021 Jul 5;219:113427.

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