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539185 Proteasome Inhibitor XX, GL5 - CAS 146304-91-8 - Calbiochem

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      Overview

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      146304-91-8C₈H₇NO₂S₃
      Description
      Overview

      This product has been discontinued.



      A cell-permeable thienyl-oxathiazolone compound that effectively kills non-replicating Mycobacterium tuberculosis (~320- or 12,600-fold drop in BCG titre over 4 days by 50 µM GL5 with or without 50 µM DETA-NO, respectively) by selectively inhibiting its proteasome activity (by ~90% over 4 hours with 50 µM GL5) in a substrate-competitive and irreversible manner, while exhibiting little activity against trypsin, cathepsin B, MMP-2, or human 20S proteasome β1/2/5. GL5 displays no antibacterial activity against M. avium-intracellulare, Staphylococcus aureus, Salmonella enterica var. Typhimurium, or Pseudomonas aeruginosa. Although GL5 is known to reversibly inhibit α-chymotrypsin (Ki = 0.064 µM), it exerts no apparent toxicity to human or monkey cells. GL5 is reasonably stable in RPMI medium (t1/2 = 110 mins at 37°C) albeit its moderate chemical reactivity toward glutathione (12.7% over 30 min at pH 7.0, RT; 10 µM GL5 and 25 µM GSH).

      Catalogue Number539185
      Brand Family Calbiochem®
      Synonyms5-(5-Methyl-2-(methylthio)thiophen-3-yl)-1,3,4-oxathiazol-2-one
      References
      ReferencesLin. G., et al. 2009. Nature 461, 621.
      Product Information
      CAS number146304-91-8
      FormBrown solid
      Hill FormulaC₈H₇NO₂S₃
      Chemical formulaC₈H₇NO₂S₃
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      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 -20°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
      Catalogue Number GTIN
      539185 0

      Documentation

      Proteasome Inhibitor XX, GL5 - CAS 146304-91-8 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Proteasome Inhibitor XX, GL5 - CAS 146304-91-8 - Calbiochem Certificates of Analysis

      TitleLot Number
      539185

      References

      Reference overview
      Lin. G., et al. 2009. Nature 461, 621.
      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.

      Revision18-April-2011 RFH
      Synonyms5-(5-Methyl-2-(methylthio)thiophen-3-yl)-1,3,4-oxathiazol-2-one
      DescriptionA cell-permeable thienyl-oxathiazolone compound that effectively kills non-replicating Mycobacterium tuberculosis (~320- or 12,600-fold drop in BCG titre over 4 days by 50 µM GL5 with or without 50 µM DETA-NO, respectively) by selectively inhibiting its proteasome activity (by ~90% over 4 hours with 50 µM GL5) in a substrate-competitive and irreversible manner, while exhibiting little activity against trypsin, cathepsin B, MMP-2, or human 20S proteasome β1/2/5. GL5 displays no antibacterial activity against M. avium-intracellulare, Staphylococcus aureus, Salmonella enterica var. Typhimurium, or Pseudomonas aeruginosa. Although GL5 is known to reversibly inhibit α-chymotrypsin (Ki = 0.064 µM), it exerts no apparent toxicity to human or monkey cells. GL5 is reasonably stable in RPMI medium (t1/2 = 110 mins at 37°C) albeit its moderate chemical reactivity toward glutathione (12.7% over 30 min at pH 7.0, RT; 10 µM GL5 and 25 µM GSH).
      FormBrown solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number146304-91-8
      Chemical formulaC₈H₇NO₂S₃
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (10 mg/ml)
      Storage Protect from light
      -20°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
      ReferencesLin. G., et al. 2009. Nature 461, 621.