5.08738

Palmostatin B

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

• Synonyme(s) : InSolution APT1 Inhibitor, palmostatin B, APT1 Inhibitor
• Formule empirique (notation de Hill): C₂₃H₃₆O₄
• Poids moléculaire : 376.53
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: liquid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• Température de stockage: −70°C

Description

Description générale

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.

Actions biochimiques/physiologiques

Primary Target
APT1

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Forme physique

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.

Autres remarques

Dekker, F. and Hedberg, C. 2011. Bioorg. Med. Chem. Lett.19, 1376.

Dekker, F., et al. 2010. Nat. Chem. Biol.6, 449.

Informations légales

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