5.08738

Palmostatin B

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

• 別名: InSolution APT1 Inhibitor, palmostatin B, APT1 Inhibitor
• 実験式（ヒル表記法）: C₂₃H₃₆O₄
• 分子量: 376.53
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: liquid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• 保管温度: −70°C

詳細

詳細

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.

生物化学的／生理学的作用

Primary Target
APT1

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

物理的形状

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

再構成

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

その他情報

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

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

法的情報

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