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178501 APT1 Inhibitor, palmostatin B - Calbiochem

APT1 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.

APT1 Inhibitor, palmostatin B - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: APT1 Inhibitor

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178501
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₃H₃₆O₄

Products

Catalogue NumberPackaging Qty/Pack
178501-5MG Glass bottle 5 mg
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
Global Trade Item Number
Catalogue Number GTIN
178501-5MG 04055977204834

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