203630 Bmi1-Ring1A E3 Ligase Inhibitor, PRT4165 - CAS 31083-55-3 - Calbiochem

203630
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203630-25MG
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      Glass bottle 25 mg
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      Description
      OverviewA cell-permeable indandione compound that inhibits the Bmi1-Ring1A E3 complex ubiquitin ligase activity both in cell-free assays (by 100% against self- and Top2α ubiquitination at 25 and 50 µM, respectively) and in HeLa cells (by 100% against Bmi1 ubiquitination at 50 µM). Shown to greatly potentiate Teniposide (VM26) cancer cytotoxicity (by 10-fold in A375 and A549 cultures at 5.5 and 33 µM, respectively) by preventing Top2α degradation following VM26 treatment (100% inhibition at 50 µM in HeLa cells).
      Catalogue Number203630
      Brand Family Calbiochem®
      Synonyms2-(Pyridin-3-ylmethylene)-1H-indene-1,3(2H)-dione
      References
      ReferencesAlcganati, I., et al. 2009. PLosOne 4, e8104.
      Product Information
      CAS number31083-55-3
      FormYellow powder
      Hill FormulaC₁₅H₉NO₂
      Chemical formulaC₁₅H₉NO₂
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetBMI1/RING1A
      Purity≥99% 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 (-207deg;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

      Bmi1-Ring1A E3 Ligase Inhibitor, PRT4165 - CAS 31083-55-3 - Calbiochem Certificates of Analysis

      TitleLot Number
      203630

      References

      Reference overview
      Alcganati, I., et al. 2009. PLosOne 4, e8104.
      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.

      Revision06-September-2013 JSW
      Synonyms2-(Pyridin-3-ylmethylene)-1H-indene-1,3(2H)-dione
      DescriptionA cell-permeable indandione compound that inhibits the activity of the E3 ubiquitin ligase complex Bmi1-Ring1A both in cell-free assays (complete inhibition of self- and Top2α ubiquitination with 25 and 50 µM PRT4165, respectively) and in HeLa cells (complete inhibition of Bmi1 ubiquitination by 50 µM PRT4165; 5 h incubation). Modifies the cellular localization of Bmi1 without affecting its expression levels. Shown to greatly potentiate Teniposide (VM26) cancer cytotoxicity (by 10-fold in A375 melanoma and A549 lung cancer cultures with 5.5 and 33 µM PRT4165, respectively) by preventing Top2α degradation following VM26 treatment (100% inhibition with 50 µM PRT4165 after 4 h 100 µM VM26 treatment in HeLa cells).
      FormYellow powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number31083-55-3
      Chemical formulaC₁₅H₉NO₂
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-207deg;C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesAlcganati, I., et al. 2009. PLosOne 4, e8104.