5.08738

Palmostatin B

InSolution, ≥95%, 50 mM in DMSO, APT1 inhibitor

• Synonym(s): InSolution APT1 Inhibitor, palmostatin B, APT1 Inhibitor
• Empirical Formula (Hill Notation): C₂₃H₃₆O₄
• Molecular Weight: 376.53
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• storage temp.: −70°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.

Biochem/physiol Actions

Primary Target
APT1

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Physical form

A 50 mM (2 mg/106.23 µL) sterile-filtered solution of APT1 Inhibitor, palmostatin B (Cat. No. 178501). in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 3 months at -20°C.

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