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。
| 生物活性 | GL0388 is aBaxactivator that results inBaxinsertion into mitochondrial membrane. GL0388 shows antiproliferative activities against variouscancercells, withIC50s of 0.299-1.57 μM. GL0388 activatesBaxand induce Bax-mediatedapoptosis. GL0388 suppresses breastcancerxenograft tumor growth in vivo[1]. |
| IC50& Target[1] | |
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].
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. |
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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].
| 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. |
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| 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. |
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