178501
APT1 Inhibitor, palmostatin B
The APT1 Inhibitor, palmostatin B controls the biological activity of APT1.
Synonym(s):
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
Recommended Products
Quality Level
Assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 100 mg/mL
shipped in
wet ice
storage temp.
−20°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. Also available as a 50 mM solution in DMSO (Cat. No. 508738).
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
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
Storage Class Code
11 - Combustible Solids
WGK
WGK 2
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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Jary Y Delgado et al.
Frontiers in molecular neuroscience, 13, 10-10 (2020-04-02)
The post-synaptic density protein 95 (PSD-95) plays a central role in excitatory synapse development and synaptic plasticity. Phosphorylation of the N-terminus of PSD-95 at threonine 19 (T19) and serine 25 (S25) decreases PSD-95 stability at synapses; however, a molecular mechanism
Gonzalo P Solis et al.
Nature communications, 13(1), 2072-2072 (2022-04-21)
Peripheral membrane proteins (PMPs) associate with cellular membranes through post-translational modifications like S-palmitoylation. The Golgi apparatus is generally viewed as the transitory station where palmitoyl acyltransferases (PATs) modify PMPs, which are then transported to their ultimate destinations such as the
I Castanon et al.
Nature communications, 11(1), 3317-3317 (2020-07-06)
Oriented cell division is a fundamental mechanism to control asymmetric stem cell division, neural tube elongation and body axis extension, among other processes. During zebrafish gastrulation, when the body axis extends, dorsal epiblast cells display divisions that are robustly oriented
Karen Rosier et al.
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Deficiency of the serine hydrolase prolyl endopeptidase-like (PREPL) causes a recessive metabolic disorder characterized by neonatal hypotonia, feeding difficulties, and growth hormone deficiency. The pathophysiology of PREPL deficiency and the physiological substrates of PREPL remain largely unknown. In this study
Zhenxing Zhang et al.
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Glucose transporter GLUT1 is a transmembrane protein responsible for the uptake of glucose into the cells of many tissues through facilitative diffusion. Plasma membrane (PM) localization is essential for glucose uptake by GLUT1. However, the mechanism underlying GLUT1 PM localization
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