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529661 Procaspase-3 Activator, PAC-1

529661
  
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      Overview

      Replacement Information
      Description
      Overview

      This product has been discontinued.





      A cell-permeable allylsalicylidine hydrazone compound that activates procaspase-3 (EC50 = 220 nM) by overcoming the safety-catch-mediated suppression of caspase autoactivation. Substitution of any of the three aspartate residues in the enzyme′s safety-catch region greatly reduces the in vitro activation efficiency (EC50 = 2.77 µM, 113 µM, and 131 µM for mutant procaspase-3 with DAD, DDA, and ADD sequence, respectively; EC50 = 4.5 µM for wild-type procaspase-7 with DTD sequence) and the potency of apoptosis induction by PAC-1 in various cells strongly correlates with procaspase-3 cellular expression levels. Shown to induce tumor retardation and regression in several murine xenograft models in a dose-dependent manner in vivo.
      Catalogue Number529661
      Brand Family Calbiochem®
      Synonyms(4-Benzylpiperazino)acetic acid-(3-allyl-2-hydroxybenzylidene)hydrazide, PAC-1
      References
      ReferencesPutt, K.S., et al. 2006. Nat. Chem. Biol. 2, 543.
      Product Information
      CAS number315183-21-2
      FormYellow solid
      Hill FormulaC₂₃H₂₈N₄O₂
      Chemical formulaC₂₃H₂₈N₄O₂
      Structure formula ImageStructure formula Image
      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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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 3 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
      529661 0

      Documentation

      Procaspase-3 Activator, PAC-1 Certificates of Analysis

      TitleLot Number
      529661

      References

      Reference overview
      Putt, K.S., et al. 2006. Nat. Chem. Biol. 2, 543.
      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
      Synonyms(4-Benzylpiperazino)acetic acid-(3-allyl-2-hydroxybenzylidene)hydrazide, PAC-1
      DescriptionA cell-permeable allylsalicylidine hydrazone compound that activates procaspase-3 (EC50 = 220 nM) by overcoming the safety-catch-mediated suppression of caspase autoactivation. Substitution of any of the three aspartate residues in the enzyme′s safety-catch region greatly reduces the in vitro activation efficiency (EC50 = 2.77 µM, 113 µM, and 131 µM for mutant procaspase-3 with DAD, DDA, and ADD sequence, respectively; EC50 = 4.5 µM for wild-type procaspase-7 with DTD sequence) and the potency of apoptosis induction by PAC-1 in various cells strongly correlates with procaspase-3 cellular expression levels. Shown to induce tumor retardation and regression in several murine xenograft models in a dose-dependent manner in vivo.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number315183-21-2
      Chemical formulaC₂₃H₂₈N₄O₂
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml), Ethanol (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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesPutt, K.S., et al. 2006. Nat. Chem. Biol. 2, 543.