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经验配方 C₂₃H₃₆O₄ 描述 概述 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. Also available as a 50 mM solution in DMSO (Cat. No. 508738). 产品目录编号 178501 品牌系列 Calbiochem®
同义词 APT1 Inhibitor 参考 参考 Dekker, F. and Hedberg, C. 2011. Bioorg. Med. Chem. Lett. 19, 1376.
Dekker, F., et al. 2010. Nat. Chem. Biol. 6, 449.产品信息 形式 Off-white solid Hill配方 C₂₃H₃₆O₄ 化学配方 C₂₃H₃₆O₄ Molar Mass 376.53 结构配方图像 生物信息 纯度 ≥95% by HPLC 理化信息 溶解度 DMSO 储存和货运信息 货运代码 Shipped with Blue Ice or with Dry Ice
毒性 Standard Handling
储存 -20°C
避光 Protect from light
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
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