5.08738
Palmostatin B
InSolution, ≥95%, 50 mM in DMSO, APT1 inhibitor
Synonym(s):
InSolution APT1 Inhibitor, palmostatin B, APT1 Inhibitor
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About This Item
Empirical Formula (Hill Notation):
C23H36O4
Molecular Weight:
376.53
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
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
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.
Biochem/physiol Actions
Primary Target
APT1
APT1
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Physical form
A 50 mM (2 mg/106.23 µL) sterile-filtered solution of APT1 Inhibitor, palmostatin B (Cat. No. 178501). in DMSO.
Reconstitution
Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 3 months at -20°C.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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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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