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533980 EMT Pathways Inhibitor, C19

A cell-permeable, bioavailable, potent and reversible multi EMT (Hippo, Wnt and TGFβ) pathway inhibitor. Blocks cancer cell migration and inhibits melanoma tumor growth.

EMT Pathways Inhibitor, C19 : FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 4-(4-(3,4-Dichlorophenyl)-1,2,5-thiadiazol-3-yloxy)butan-1-ol, Epithelial-Mesenchymal Transition (EMT) Pathways Inhibitor, AMPK Signaling Activator XV; Hippo Pathway Inhibitor, Wnt Pathway Inhibitor XXIV

Primary Target: multiple pathways involved in epithelial-mesenchymal transition
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      Aperçu

      Replacement Information

      Tableau de caractéristiques principal

      Empirical Formula
      C₁₂H₁₂Cl₂N₂O₂S
      Description
      OverviewA cell-permeable, bioavailable, thiadiazolyloxybutanol compound that acts as a potent and reversible inhibitor of multiple pathways involved in epithelial-mesenchymal transition (EMT; IC50 < 2 µM for Hippo signaling in HEK293 cells transfected with TEAD luciferase reporter system 8XGTIIC). Also shown to be an effective inhibitor of Wnt and TGF-β signaling pathways. Induces GSK-3β-mediated degradation of TAZ by activating Hippo kinases Mst1 and Lats1. Shown to be about 10-fold more potent than AICAR (Cat. no. 123040) in inducing phosphorylation (Thr172) and activation of AMPK leading to autophagy. However, it does not appear to induce apoptosis in cells. Shown to increase degradation of nuclear b-catenin and increase the level of cytosolic β-catenin in multiple cancer cell lines (WM266, SW480, and MCF7) and suppresses the expression of various genes associated with EMT (Zeb1, Snail, Hes, Myc and Cyclin D). Inhibits the growth of WM266 melanoma tµMor xenografts in mice (20 mg/kg, i.p., X 3 in 30 days) once in 3 days for 30 days) without affecting their body weights.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533980
      Brand Family Calbiochem®
      Synonyms4-(4-(3,4-Dichlorophenyl)-1,2,5-thiadiazol-3-yloxy)butan-1-ol, Epithelial-Mesenchymal Transition (EMT) Pathways Inhibitor, AMPK Signaling Activator XV; Hippo Pathway Inhibitor, Wnt Pathway Inhibitor XXIV
      References
      ReferencesBasu, D., et al. 2014. Mol. Cancer Ther. 13, 1457.
      Product Information
      FormOff-white solid
      Hill FormulaC₁₂H₁₂Cl₂N₂O₂S
      Chemical formulaC₁₂H₁₂Cl₂N₂O₂S
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Targetmultiple pathways involved in epithelial-mesenchymal transition
      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
      533980 0

      Documentation

      EMT Pathways Inhibitor, C19 FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Basu, D., et al. 2014. Mol. Cancer Ther. 13, 1457.
      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.

      Revision26-June-2017 JSW
      Synonyms4-(4-(3,4-Dichlorophenyl)-1,2,5-thiadiazol-3-yloxy)butan-1-ol, Epithelial-Mesenchymal Transition (EMT) Pathways Inhibitor, AMPK Signaling Activator XV; Hippo Pathway Inhibitor, Wnt Pathway Inhibitor XXIV
      DescriptionA cell-permeable thiadiazolyloxybutanol compound that inhibits epithelial-mesenchymal transition-(EMT) dependent cancer proliferation (% viability by MTT = 2.7%/RPMI-8226, 12%/MCF7, 15%/WM266, 32%/SK-Mel-28, 44%/WM115, 63%/SW480 vs. 80%/normal fibroblast; 5 µM C19 for 96 h) due to autophagy, but not apoptosis, induction by blocking both basal & ligands-stimulated Hippo, Wnt, and TGF-β pathway signalings (IC50 <2.5 µM in 293-based reporter assays; 24 h treatment) via simultaneous AMPK, Lats1 & Mst1 activation/phosphorylation induction (Effective conc <5 µM), resulting in downstream GSK-3β activation/dephosphorylation and GSK-3β destruction complex-mediated Hippo pathway transducer TAZ degradation. In addition to inhibiting WM266 migration and cellular EMT genes expression (Zeb1, Snail, Hes, Myc and Cyclin D) in vitro, C19 is also reported to effectively suppress WM266-derived tµMor growth in mice in vivo (% suppression/i.p. dosage in mg/kg = 86/20, 60%/10, and 35%/5 on d29 post cancer cells inoculation; C19 injections applied on d15/d18/d21 post cancer cells inoculation) without noticeable adverse effect to the animals. Compared to AICAR (Cat. no. 123040), AMPK is at least 10-times more potent in inducing AMPK Thr172 phosphorylation induction both in live WM266 cultures and in cell-free immune complex kinase assays.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₂H₁₂Cl₂N₂O₂S
      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
      ReferencesBasu, D., et al. 2014. Mol. Cancer Ther. 13, 1457.