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533259 FOXM1 Inhibitor III, FDI-6 - Calbiochem

533259
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₉H₁₁F₄N₃OS₂

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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
      Quality LevelMQ100
      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 MSDS

      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.