533980 EMT Pathways Inhibitor, C19

533980
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₂H₁₂Cl₂N₂O₂S

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      5.33980.0001
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          Glass bottle 10 mg
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          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
          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

          Documentation

          EMT Pathways Inhibitor, C19 SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Basu, D., et al. 2014. Mol. Cancer Ther. 13, 1457.
          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.

          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 +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
          ReferencesBasu, D., et al. 2014. Mol. Cancer Ther. 13, 1457.