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533259 FOXM1 Inhibitor III, FDI-6 - CAS 313380-27-7 - Calbiochem

FOXM1 inhibitor FDI-6; NCGC00099374

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: FDI6, Forkhead Domain Inhibitory Compound 6, NCGC00099374

Primary Target: FOXM1
533259
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Aperçu

Replacement Information

Tableau de caractéristiques principal

CAS #Empirical Formula
313380-27-7C₁₉H₁₁F₄N₃OS₂

Products

RéférenceConditionnement Qté
5332590001 Flacon en verre 10 mg
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
CAS number313380-27-7
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
Global Trade Item Number
Référence GTIN
5332590001 04055977281514

Documentation

FOXM1 Inhibitor III, FDI-6 - CAS 313380-27-7 - Calbiochem FDS

Titre

Fiche de données de sécurité des matériaux (FDS) 

Références bibliographiques

Aperçu de la référence bibliographique
Gormally , M.V., et al. 2014. Nat. Commun. 5, 5156.
Fiche technique

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
CAS number313380-27-7
Chemical formulaC₁₉H₁₁F₄N₃OS₂
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
+2°C to +8°C
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.