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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 MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 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
533980
  
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Přehled

Replacement Information

Tabulka spec. kláve

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
Katalogové číslo GTIN
533980 0

Documentation

EMT Pathways Inhibitor, C19 MSDS

Title

Safety Data Sheet (SDS) 

References

Přehled odkazů
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 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.