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178501 APT1 Inhibitor, palmostatin B - Calbiochem

Overview

Key Spec Table

Empirical Formula
C₂₃H₃₆O₄

Products

Catalogue NumberPackaging Qty/Pack
178501-5MGCN 玻璃瓶 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
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
Global Trade Item Number
Catalogue Number GTIN
178501-5MGCN 04055977204834