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メルク株式会社
目黒区下目黒1-8-1
153-8927 東京
Japan
TEL： 0120-189-390
Fax: 0120-189-350
E-mail mj_service@merckgroup.com
31 5月 2012
ローディング
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.
| 製品情報 | |||
|---|---|---|---|
| Form | Off-white solid | ||
| Protect from Light | はい | ||
| Packaged under inert gas | はい | ||
| Purity | ≥95% by HPLC | ||
| 化学式 | C23H36O4 | ||
| 保管と送付情報 | |||
|---|---|---|---|
| Storage | -20°C | ||
| Ship |
Shipped with Blue Ice or with Dry Ice
Standard Handling |
||
