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178501

Sigma-Aldrich

Palmostatin B

≥95% (HPLC), solid, APT1 inhibitor, Calbiochem®

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
NACRES:
NA.77

product name

APT1 Inhibitor, palmostatin B, The APT1 Inhibitor, palmostatin B controls the biological activity of APT1.

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.

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


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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
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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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