2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
FL-411 is a selective BRD4 inhibitor. Binding affinities of FL-411 are measured by TR-FRET against the first and second bromodomains of BRD2(1), BRD4(1), and BRD4(2) with IC50s of 24.60±0.70 μM, 0.47±0.02 μM, 0.93±0.05 μM, respectively. FL-411 possesses a good BRD4(1) inhibition activity (IC50=0.43±0.09 μM), antiproliferative activity (MCF-7, IC50=1.62±0.06 μM; MDA-MB-231, IC50=3.27±0.14 μM), and autophagic activity (42.29% in MCF-7 cells), as well as displays a low toxicity against MCF10A cells). FL-411 induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction and thus activating AMPK-mTOR-ULK1-modulated autophagic pathway in breast cancer cells.
