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 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC 50 s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo.

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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.
GL0388 (0.01-100 μM) inhibits the cell proliferation in 60 human tumor cell lines, with GI550s of 0.299-1.57 μM.
GL0388 (1-10 μM; 48 h) significantly upregulates the cleaved PARP-1 and cleaved caspase 3 in MDA-MB-231 cells.
GL0388 (0.1-1 μM; 24 h) inhibits the colony formation and invasion of breast cancer cells.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

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[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.