178501 APT1 Inhibitor, palmostatin B - Calbiochem

178501
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₃H₃₆O₄

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178501-5MG
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      Glass bottle 5 mg
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      Description
      OverviewA cell-permeable, beta-lactone acyl protein thioesterase 1 (APT1) inhibitor (IC50 = 0.67 µM, in an enzymatic assay) that is shown to specifically block Ras depalmitoylation, without affecting Ras acylation, in MDCK cells, both in vitro and in vivo. It induces a marked redistribution of NRas to endomembranes (1 µM) without notable cytotoxicity, and is shown to elicit a loss of the precise steady-state localization of palmitoylated Ras proteins in the same cell line. At 50 µM, this inhibitor displays a partial phenotypic reversion in oncogenic HRasG12V-transformed fibroblasts. Furthermore, it demonstrates selectivity for APT1 over phospholipase A1, A2, Cβ and D. It's inhibitory effect is demonstrated to be consistent with that of APT1 downregulation by siRNA. Also available as a 50 mM solution in DMSO (Cat. No. 508738).
      Catalogue Number178501
      Brand Family Calbiochem®
      SynonymsAPT1 Inhibitor
      References
      ReferencesDekker, F. and Hedberg, C. 2011. Bioorg. Med. Chem. Lett. 19, 1376.
      Dekker, F., et al. 2010. Nat. Chem. Biol. 6, 449.
      Product Information
      FormOff-white solid
      Hill FormulaC₂₃H₃₆O₄
      Chemical formulaC₂₃H₃₆O₄
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationAPT1 Inhibitor, Palmostatin B is a cell-permeable inhibitor of acyl protein thioesterase 1 (IC50 = 0.67 µM) that specifically block Ras depalmitoylation, without affecting Ras acylation.
      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 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

      Documentation

      APT1 Inhibitor, palmostatin B - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      APT1 Inhibitor, palmostatin B - Calbiochem Certificates of Analysis

      TitleLot Number
      178501

      References

      Reference overview
      Dekker, F. and Hedberg, C. 2011. Bioorg. Med. Chem. Lett. 19, 1376.
      Dekker, F., et al. 2010. Nat. Chem. Biol. 6, 449.
      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.

      Revision01-September-2011 RFH
      SynonymsAPT1 Inhibitor
      DescriptionA cell-permeable, beta-lactone acyl protein thioesterase 1 (APT1) inhibitor (IC50 = 0.67 µM, in an enzymatic assay) that is shown to specifically block Ras depalmitoylation, without affecting Ras acylation, in MDCK cells, both in vitro and in vivo. It induces a marked redistribution of NRas to endomembranes (1 µM) without notable cytotoxicity, and is shown to elicit a loss of the precise steady-state localization of palmitoylated Ras proteins in the same cell line. At 50 µM, this inhibitor displays a partial phenotypic reversion in oncogenic HRasG12V-transformed fibroblasts. Furthermore, it demonstrates selectivity for APT1 over phospholipase A1, A2, Cβ and D. It's inhibitory effect is demonstrated to be consistent with that of APT1 downregulation by siRNA.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₃H₃₆O₄
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage -20°C
      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.
      Toxicity Standard Handling
      ReferencesDekker, F. and Hedberg, C. 2011. Bioorg. Med. Chem. Lett. 19, 1376.
      Dekker, F., et al. 2010. Nat. Chem. Biol. 6, 449.