178501

Palmostatin B

≥95% (HPLC), solid, APT1 inhibitor, Calbiochem^®

• Synonym(s): APT1 Inhibitor, palmostatin B, APT1 Inhibitor
• Empirical Formula (Hill Notation): C₂₃H₃₆O₄
• Molecular Weight: 376.53
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥95% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Product Name: APT1 Inhibitor, palmostatin B, The APT1 Inhibitor, palmostatin B controls the biological activity of APT1.
• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: off-white
• solubility: DMSO: 100 mg/mL
• shipped in: wet ice
• storage temp.: −20°C

Description

General description

A 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).

Packaging

Packaged under inert gas

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable