5.08738

Palmostatin B

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

• Sinônimo(s): InSolution APT1 Inhibitor, palmostatin B, APT1 Inhibitor
• Fórmula empírica (Notação de Hill): C₂₃H₃₆O₄
• Peso molecular: 376.53
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• forma: liquid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• temperatura de armazenamento: −70°C

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

Primary Target
APT1

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

forma física

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

Reconstituição

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

Outras notas

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

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

Informações legais

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