5.08738
Palmostatin B
≥95% (HPLC), APT1 inhibitor, liquid
別名:
InSolution APT1 Inhibitor, palmostatin B, APT1 Inhibitor
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この商品について
実験式（ヒル表記法）:
C23H36O4
分子量:
376.53
UNSPSC Code:
12352200
NACRES:
NA.77
製品名
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
Primary Target
APT1
APT1
Disclaimer
Toxicity: Standard Handling (A)
General description
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.
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
Packaged under inert gas
Physical form
A 50 mM (2 mg/106.23 µL) sterile-filtered solution of APT1 Inhibitor, palmostatin B (Cat. No. 178501). in DMSO.
Preparation Note
Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
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
グローバルトレードアイテム番号
| カタログ番号 | GTIN |
|---|---|
| 5.08738.0001 | 04055977261356 |
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