178501 APT1 Inhibitor, palmostatin B - Calbiochem

178501
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₃H₃₆O₄

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      178501-5MG
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      Stocked 
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.