|3-氨基-N-(4-氟苯基)-6-(噻吩-2-基)-4-(三氟甲基)噻吩并[2,3-b]吡啶-2-甲酰胺|CsnPharm

CAS No.: 313380-27-7

FDI-6 Catalog No. CSN24469

Synonyms: NCGC00099374

FDI-6 is an inhibitor of FOXM1 that block DNA binding. It act by specifically downregulating FOXM1-activated genes.

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靶点选择性

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实验方案

技术信息

生物活性

描述FOXM1 (forkhead box protein M1) is a critical proliferation-associated transcription factor that is widely spatiotemporally expressed during the cell cycle. It is closely involved with the processes of cell proliferation, self-renewal, and tumorigenesis. In most human cancers, FOXM1 is overexpressed, and this indicates a poor prognosis for cancer patients^[1]. FDI-6 (forkhead domain inhibitor-6) is an inhibitor of FOXM1. FDI-6 binds directly to FOXM1 protein, to displace FOXM1 from genomic targets in MCF-7 breast cancer cells, and induce concomitant transcriptional down-regulation^[2]. MDA-MB-231 ER-negative breast and PEO-1 ovarian cancer cells are sensitive to FDI-6 in cell viability assays (GI₅₀=21.8 μM and 18.1 μM, respectively) and exhibit comparable down-regulation of CDC25B after a 3h treatment with FDI-6^[2]. 24h after 10, 20 μM FDI-6 treatment, the apoptosis rate in Hep-2 cells was elevated and the ability of cell invasion and migration was inhibited in a dose-dependent manner. In the nuclear, FoxM1 protein level decreased along with the ascent of FDI-6 concentration^[3].
参考文献

[1] Liao GB, Li XZ, Zeng S, Liu C, Yang SM, Yang L, Hu CJ, Bai JY. Regulation of the master regulator FOXM1 in cancer. Cell Commun Signal. 2018 Sep 12;16(1):57. doi: 10.1186/s12964-018-0266-6. PMID: 30208972; PMCID: PMC6134757.
[2] Gormally MV, Dexheimer TS, Marsico G, Sanders DA, Lowe C, Matak-Vinković D, Michael S, Jadhav A, Rai G, Maloney DJ, Simeonov A, Balasubramanian S. Suppression of the FOXM1 transcriptional programme via novel small molecule inhibition. Nat Commun. 2014 Nov 12;5:5165. doi: 10.1038/ncomms6165. PMID: 25387393; PMCID: PMC4258842.
[3] Liu Y, Zhu L, Wen T, Wan J, Lei Y, Chen H. [Forkhead domain inhibitor-6 (FDI-6) increases apoptosis and inhibits invasion and migration of laryngeal carcinoma cells by down-regulating nuclear FoxM1]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2017 May;33(5):611-616. Chinese. PMID: 28502298.

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
- 2.2861 mL
- 11.4303 mL
- 22.8606 mL
- 5 mM
- 0.4572 mL
- 2.2861 mL
- 4.5721 mL
- 10 mM
- 0.2286 mL
- 1.1430 mL
- 2.2861 mL

技术信息

CAS号

313380-27-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H11F4N3OS2

运输

蓝冰

分子量

437.43

别名

NCGC00099374

溶解度

DMSO	86.0 mg/mL (196.6 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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