5.08738
Palmostatin B
InSolution, ≥95%, 50 mM in DMSO, APT1 inhibitor
Synonim(y):
InSolution APT1 Inhibitor, palmostatin B, APT1 Inhibitor
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About This Item
Wzór empiryczny (zapis Hilla):
C23H36O4
Masa cząsteczkowa:
376.53
Kod UNSPSC:
12352200
Polecane produkty
Poziom jakości
Próba
≥95% (HPLC)
Postać
liquid
producent / nazwa handlowa
Calbiochem®
warunki przechowywania
OK to freeze
avoid repeated freeze/thaw cycles
desiccated (hygroscopic)
protect from light
temp. przechowywania
−70°C
Opis ogólny
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.
Działania biochem./fizjol.
Primary Target
APT1
APT1
Opakowanie
Packaged under inert gas
Ostrzeżenie
Toxicity: Standard Handling (A)
Postać fizyczna
A 50 mM (2 mg/106.23 µL) sterile-filtered solution of APT1 Inhibitor, palmostatin B (Cat. No. 178501). in DMSO.
Rekonstytucja
Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 3 months at -20°C.
Inne uwagi
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.
Informacje prawne
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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Dokumenty związane z niedawno zakupionymi produktami zostały zamieszczone w Bibliotece dokumentów.
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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