FDI-6

• CAT Number: I012642
• CAS Number: 313380-27-7
• Molecular Formula: C19H11F4N3OS2
• Molecular Weight: 437.43
• Purity: ≥95%
• Synonyms: 3-amino-N-(4-fluorophenyl)-6-thiophen-2-yl-4-(trifluoromethyl)thieno[2,3-b]pyridine-2-carboxamide
• InChI: InChI=1S/C19H11F4N3OS2/c20-9-3-5-10(6-4-9)25-17(27)16-15(24)14-11(19(21,22)23)8-12(26-18(14)29-16)13-2-1-7-28-13/h1-8H,24H2,(H,25,27)
• InChIKey: ZATJMMZPGVDUOM-UHFFFAOYSA-N
• SMILES: C1=CSC(=C1)C2=NC3=C(C(=C2)C(F)(F)F)C(=C(S3)C(=O)NC4=CC=C(C=C4)F)N

FDI-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.
FDI-6 is characterized in depth and is shown to bind directly to FOXM1 protein, to displace FOXM1 from genomic targets in MCF-7 breast cancer cells, and induce concomitant transcriptional down-regulation. 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 3 h treatment with FDI-6. The transcription factor FOXM1 regulates a network of proliferation-associated genes critical to mitotic spindle assembly, chromosome segregation, and G2/M transition, with depletion leading to cell cycle arrest. Importantly, aberrant up-regulation of FOXM1 has been shown to be a key driver of cancer progression and has been proposed as an initiating factor of oncogenesis[1].

Reference

[1]. Gormally MV, et al. Suppression of the FOXM1 transcriptional programme via novel small molecule inhibition. Nat Commun. 2014 Nov 12;5:5165.
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