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

203630
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      Overview

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      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      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
          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

          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.