产品名称
Palmostatin B, InSolution, ≥95%, 50 mM in DMSO, APT1 inhibitor
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
Quality Level
Biochem/physiol Actions
主要靶标
APT1
APT1
Disclaimer
毒性：标准处理（A）
General description
一种细胞可渗透的β-内酯酰基蛋白硫酯酶1（APT1）抑制剂（在酶促测定中IC50 = 0.67 µM），在体外和体内均能特异性阻断MDCK细胞中的Ras去棕榈酰化而不影响Ras酰化。它诱导NRas显著重新分布到内膜（1 µM），而没有明显的细胞毒性，并且显示出在同一细胞系中引起棕榈酰化Ras蛋白精确稳态定位的丧失。在50 µM时，该抑制剂在致癌的HRasG12V转化的成纤维细胞中显示出部分表型逆转。此外，它证明了APT1对磷脂酶A1、A2、Cβ和D的选择性。其′抑制作用与siRNA下调APT1的抑制作用一致。
Other Notes
Dekker, F. and Hedberg, C. 2011.Bioorg.Med. Chem. Lett.19, 1376.
Dekker, F., et al. 2010.Nat. Chem. Biol.6, 449.
Dekker, F., et al. 2010.Nat. Chem. Biol.6, 449.
Packaging
用惰性气体包装
Physical form
50 mM (2 mg/106.23 µL) APT1抑制剂（palmostatin B，目录号178501）在DMSO中的无菌过滤溶液。
Preparation Note
初次融化后，等分并冷冻（-20°C）。分装后在-20°C下可稳定保存3个月。
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Frank J Dekker et al.
Bioorganic & medicinal chemistry, 19(4), 1376-1380 (2010-12-07)
The H- and N-Ras GTPases are prominent examples of proteins, whose localizations and signalling capacities are regulated by reversible palmitoylations and depalmitoylations. Recently, the novel small molecule inhibitor palmostatin B has been described to inhibit Ras depalmitoylation and to revert
Frank J Dekker et al.
Nature chemical biology, 6(6), 449-456 (2010-04-27)
Cycles of depalmitoylation and repalmitoylation critically control the steady-state localization and function of various peripheral membrane proteins, such as Ras proto-oncogene products. Interference with acylation using small molecules is a strategy to modulate cellular localization--and thereby unregulated signaling--caused by palmitoylated
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