533259 FOXM1 Inhibitor III, FDI-6 - Calbiochem

533259
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₉H₁₁F₄N₃OS₂

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      5.33259.0001
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          Glass bottle 10 mg
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          Description
          Overview A cell-permeable thienopyridinylcarboxamide compound that selectively and directly binds to forkhead box M1 (FOXM1) in a 1:1 stoichiometry and reversibly blocks its DNA binding activity (IC50 = 22.5 µM). Does not affect the transcriptional activity of FOXA1, FOXA2, FOXP2, and GATA1 in any significant manner. Shown to suppress the expression of FOXM1 target genes and block the proliferation of FOXM1 expressing breast cancer cells (GI50 = 18 µM for MCF-7 and MDA-MB-231 cells and 21.8 µM for PEO-1 cells). Unlike thiostrepton (Cat. No. 598226), it displays minimal off-target effects and does not affect 20S proteasomal activity.
          Catalogue Number533259
          Brand Family Calbiochem®
          SynonymsFDI6, Forkhead Domain Inhibitory Compound 6, NCGC00099374
          References
          ReferencesGormally , M.V., et al. 2014. Nat. Commun. 5, 5156.
          Product Information
          FormYellow solid
          Hill FormulaC₁₉H₁₁F₄N₃OS₂
          Chemical formulaC₁₉H₁₁F₄N₃OS₂
          ReversibleY
          Applications
          Biological Information
          Primary TargetFOXM1
          Purity≥98% by HPLC
          Physicochemical Information
          Cell permeableY
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          FOXM1 Inhibitor III, FDI-6 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Gormally , M.V., et al. 2014. Nat. Commun. 5, 5156.
          Data Sheet

          Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

          Revision01-March-2016 JSW
          SynonymsFDI6, Forkhead Domain Inhibitory Compound 6, NCGC00099374
          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.
          FormYellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₉H₁₁F₄N₃OS₂
          Purity≥98% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesGormally , M.V., et al. 2014. Nat. Commun. 5, 5156.