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CAS No.: 2118944-88-8

FL-411 Catalog No. CSN21184

Synonyms: BRD4-IN-1

FL-411 selectively inhibits BRD4 with an IC50 of 0.43 ± 0.09 μM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Bromodomain-containing protein 4 (BRD4) belongs to the bromodomain and extra-terminal (BET) protein family, functions as an epigenetic and transcriptional regulatory. FL-411 shows potent inhibitory activity against BRD4 with an IC₅₀ value of 0.43 µM. It also inhibited the proliferation of MCF-7 cells and MDA-MB-231 cells with IC₅₀ values of 1.62 μM and 3.27 μM, respectively. In MCF-7 and MDA-MB-231 cells treated with 1.5 or 3 μM FL-411, the expression of BRD4 and its downstream target c-Myc were greatly inhibited as compared to the control group, whereas the phosphorylation of AMPKα at thr172 site was activated. FL-411 also augmented the interaction between p53 and AMPK, but attenuated the interaction between BRD4 and p53 in MCF-7 cells. FL-411 at 1.5 or 3 μM downregulated the expression levels of p-Akt (ser473), p-Akt (thr308), and p-mTOR (ser2448) in MCF-7 or MDA-MB-231 cells, while the expressions of Akt and mTOR remained unchanged. The administration of FL-411 (25, 50, and 100 mg/kg) resulted in 80% and 76% tumor growth inhibition in mice models inoculated with MCF-7 or MDA-MB-231 cells, respectively, in a dose-dependent manner. FL-411-treated animals also showed reduced number of Ki-67 positive cells and increased LC3 expression in the tumor tissues^[1].
作用机制FL-411 is a potent and selective inhibitor of BRD4. The 3,5-dimethylphenol moiety of FL-411 penetrated into the N-acetylated lysine pocket of the enzyme, forming a direct hydrogen bond. The residues Gln85 and Pro82 contribute to the selectivity of FL-411 over BRD4.
参考文献

[1] Ouyang L, Zhang L, Liu J, Fu L, Yao D, Zhao Y, Zhang S, Wang G, He G, Liu B. Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. J Med Chem. 2017 Dec 28;60(24):9990-10012. doi: 10.1021/acs.jmedchem.7b00275. Epub 2017 Dec 7. PMID: 29172540.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9289 mL
- 14.6444 mL
- 29.2888 mL
- 5 mM
- 0.5858 mL
- 2.9289 mL
- 5.8578 mL
- 10 mM
- 0.2929 mL
- 1.4644 mL
- 2.9289 mL

技术信息

CAS号

2118944-88-8

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H19N3O2S

运输

蓝冰

分子量

341.43

别名

BRD4-IN-1

溶解度

DMSO	5.0 mg/mL (14.6 mM) warming
Water	Insoluble

动物实验配方

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