5.08738

Palmostatin B

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

• Synonym(e): InSolution APT1 Inhibitor, palmostatin B, APT1 Inhibitor
• Empirische Formel (Hill-System): C₂₃H₃₆O₄
• Molekulargewicht: 376.53
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥95% (HPLC)
• Form: liquid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• Lagertemp.: −70°C

Beschreibung

Allgemeine Beschreibung

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. Wirkung

Primary Target
APT1

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Physikalische Form

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

Rekonstituierung

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

Sonstige Hinweise

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

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

Rechtliche Hinweise

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