5.33259
FOXM1 Inhibitor III, FDI-6
Synonym(s):
FOXM1 Inhibitor III, FDI-6, FDI6, Forkhead Domain Inhibitory Compound 6, NCGC00099374
Sign In to View Organizational & Contract Pricing.
Select a Size
Change View
About This Item
Empirical Formula (Hill Notation):
C19H11F4N3OS2
CAS Number:
Molecular Weight:
437.43
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥98% (HPLC)
Quality Segment
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
SMILES string
FC(F)(F)c1c2c([s]c(c2N)C(=O)Nc4ccc(cc4)F)nc(c1)c3[s]ccc3
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)
InChI key
ZATJMMZPGVDUOM-UHFFFAOYSA-N
General description
A cell-permeable thienopyridinylcarboxamide compound that targets forkhead box M1 (FOXM1) winged helix DNA-binding domain (DBD; aa 222-360 in FOXM1c) in a 1:1 stoichiometric ratio and effectively blocking FOXM1 DBD DNA-binding activity (IC50 = 22.5 µM by EMSA; 15 nM DNA probe & 750 nM FOXM1 DBD) and displays antiproliferative activity in breast cancer cultures (GI50 = 18 µM/MCF-7, 18.1 µM/PEO-1, and 21.8 µM/MDA-MB-231 with 72 h treatment). FDI-6 culture treatment reduces FOXM1 target genes promoter occupancy (by 36%/CDC25B and 38%/CCNB1 with 6 h treatment at 40 µM in MCF-7 cultures) and overall FOXM1 chromatin association (by 43%/20 µM and 79%/40 µM in MCF-7 cultures), resulting in decreased FOXM1 target genes mRNA level (by 57%/PLK1, 55%/CDC25B, 52%/AURKB, 45%/CARM1 with 6 h treatment at 40 µM in MCF-7 cultures). Close to a 19-fold enriched FOXM1 targets is seen among downregulated mRNA species when compared to those not affected by FDI-6 treatment, while little or no enrichment is seen pertaining to targets of highly homologous FOX family transcription factors FOXA1, FOXA2, and FOXP2 among mRNAs affected by FCI-6 treatment. Unlike Thiostrepton (Cat. No. 598226), FDI-6 does not inhibit 20S proteasome activity.
FOXM1 inhibitor FDI-6; NCGC00099374
Biochem/physiol Actions
Cell permeable: yes
Primary Target
FOXM1
FOXM1
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Gormally , M.V., et al. 2014. Nat. Commun.5, 5156.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
Already Own This Product?
Find documentation for the products that you have recently purchased in the Document Library.