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575547 Tankyrase1/2 Inhibitor IV, JW55 - CAS 664993-53-7 - Calbiochem

The Tankyrase1/2 Inhibitor IV, JW55 controls the biological activity of Tankyrase1/2. This small molecule/inhibitor is primarily used for Biochemicals applications.

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Synonyme: N-(4-((4-(4-Methoxyphenyl)tetrahydro-2H-pyran-4-yl)methylcarbamoyl)phenyl)furan-2-carboxamide, TNKS1/2 Inhibitor IV, Wnt Pathway Inhibitor XVII

Primary Target: tankyrase 1 and 2
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      Übersicht

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      664993-53-7C₂₅H₂₆N₂O₅
      Description
      OverviewA cell-permeable phenylcarbamoylfuran-carboxamide compound that acts as a potent, selective, and reversible inhibitor of poly(ADP-ribosyl)ation activity of tankyrase 1 and 2 (IC50 = 1.9 and 0.83 µM, respectively). Exhibits high selectivity over PARP1 (IC50 = 20 µM). Stabilizes and increases AXIN2 levels, thereby enhancing phosphorylation and degradation of β-catenin resulting in reduced canonical Wnt signaling (IC50 = 470 nM in Wnt 3a-induced HEK293 cells transfected with ST-Luc). Shown to induce cell cycle arrest and diminish the proliferation of SW480 colorectal cancer cells (~ 5 µM). Suppresses tumor growth in tamoxifen-induced polyposis in Apc knock-out murine model (100 mg/kg, i.p.). Displays adequate human liver microsomal stability (t1/2 = 10.1 min).
      Catalogue Number575547
      Brand Family Calbiochem®
      SynonymsN-(4-((4-(4-Methoxyphenyl)tetrahydro-2H-pyran-4-yl)methylcarbamoyl)phenyl)furan-2-carboxamide, TNKS1/2 Inhibitor IV, Wnt Pathway Inhibitor XVII
      References
      ReferencesWaaler, J., et al. 2012. Cancer Res. 72, 2822.
      Product Information
      CAS number664993-53-7
      FormOff-white solid
      Hill FormulaC₂₅H₂₆N₂O₅
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality SegmentMQ100
      Applications
      Biological Information
      Primary Target tankyrase 1 and 2
      Purity≥99% 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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade ITEM Number
      Bestellnummer GTIN
      575547 0

      Documentation

      Tankyrase1/2 Inhibitor IV, JW55 - CAS 664993-53-7 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Tankyrase1/2 Inhibitor IV, JW55 - CAS 664993-53-7 - Calbiochem Analysenzertifikate

      TitelChargennummer
      575547

      Literatur

      Übersicht
      Waaler, J., et al. 2012. Cancer Res. 72, 2822.
      Datenblatt

      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.

      Revision11-October-2013 JSW
      SynonymsN-(4-((4-(4-Methoxyphenyl)tetrahydro-2H-pyran-4-yl)methylcarbamoyl)phenyl)furan-2-carboxamide, TNKS1/2 Inhibitor IV, Wnt Pathway Inhibitor XVII
      DescriptionA cell-permeable phenylcarbamoylfuran-carboxamide compound that acts as a potent, selective, and reversible inhibitor of poly(ADP-ribosyl)ation activity of tankyrase 1 and 2 (IC50 = 1.9 and 0.83 µM, respectively). Exhibits high selectivity over PARP1 (IC50 = 20 µM). Stabilizes and increases AXIN2 levels, thereby enhancing phosphorylation and degradation of β-catenin resulting in reduced canonical Wnt signaling (IC50 = 470 nM in Wnt 3a-induced HEK293 cells transfected with ST-Luc). Shown to induce cell cycle arrest and diminish the proliferation of SW480 colorectal cancer cells (~ 5 µM). Suppresses tumor growth in tamoxifen-induced polyposis in Apc knock-out murine model (100 mg/kg, i.p.). Displays adequate human liver microsomal stability (t1/2 = 10.1 min).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number664993-53-7
      Structure formulaStructure formula
      Purity≥99% HPLC
      SolubilityDMSO (100 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 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesWaaler, J., et al. 2012. Cancer Res. 72, 2822.