Fostriecin sodium salt
Chemical Name: (6R)-5,6-Dihydro-6-[(1E,3R,4R,6R,7Z,9Z,11E)-3,6,13-trihydroxy-3-methyl-4-(phosphonooxy)-1,7,9,11-tridecatetraenyl]-2H-pyran-2-one sodium salt
Purity: ≥98%
Biological Activity
Fostriecin sodium salt is a potent inhibitor of protein phosphatase types 2A (PP2A) and 4 (PP4) with IC50 values of 1.5 nM and 3 nM respectively. Also exhibits weaker inhibition of topoisomerase II (IC50 = 40 μM) and protein phosphatase type 1 (PP1) (IC50 = 131 μM) with no apparent inhibition of protein phosphatase type 2B (PP2B). Active in vivo. Originally identified as an antitumor antibiotic from Streptomyces pulveraceous.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Novel antitumor agents CI-920, PD 113,270 and PD 113,271. I. Taxonomy, fermentation and biological properties.
Tunac et al.
J.Antibiot., 1983;36:1595 -
Fostriecin, an antitumor antibiotic with inhibitory activity against serine/threonine protein phosphatases types 1 (PP1) and 2A (PP2A), is highly selective for PP2A.
Walsh et al.
FEBS Lett., 1997;416:230 -
Purification of protein phosphatase 4 catalytic subunit: inhibition by the antitumour drug fostriecin and other tumour suppressors and promoters.
Hastie and Cohen
FEBS Lett., 1998;431:357
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Citations for Fostriecin sodium salt
The citations listed below are publications that use Tocris products. Selected citations for Fostriecin sodium salt include:
7 Citations: Showing 1 - 7
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NMDAR-Activated PP1 Dephosphorylates GluN2B to Modulate NMDAR Synaptic Content.
Authors: Chiu Et al.
Cell Rep 2019;28:332
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In vivo brain GPCR signaling elucidated by phosphoproteomics.
Authors: Liu
Science 2018;360(6395):eaao4927
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Prolonged adenosine A1 receptor activation in hypoxia and pial vessel disruption focal cortical ischemia facilitates clathrin-mediated AMPA receptor endocytosis and long-lasting synaptic inhibition in rat hippocampal CA3-CA1 synapses: differential regulat
Authors: Chen Et al.
J Neurosci 2014;34:9621
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TNF-α Downregulates Inhibitory Neurotransmission through Protein Phosphatase 1-Dependent Trafficking of GABAA Receptors.
Authors: Pribiag and Stellwagen
J Neurosci 2013;33:15879
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DA-dependent tuning of striatal inhibitory synaptogenesis.
Authors: Goffin Et al.
J Neurosci 2010;30:2935
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Amphetamine modulation of long-term potentiation in the prefrontal cortex: dose dependency, monoaminergic contributions, and paradoxical rescue in hyperDArgic mutant.
Authors: Xu Et al.
J Neurosci 2010;115:1643
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HyperDArgic tone erodes prefrontal long-term potential via a D2 receptor-operated protein phosphatase gate.
Authors: Xu Et al.
J Neurosci 2009;29:14086
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fostriecin for PP2A/4 (Fos, 1 μM)
HL-1 cardiomyocytes were treated with 100 nM fostriecin, 100 nM Okadaic acid or 50 nM 8-bromo-cAMP for 30 min followed by Western blot analysis for pCaMKII expression. Fostriecin slightly increased phosphorylation of CaMKII; indicating role of PP2A in CaMKII dephosphorylation.
I used fostriecin to investigate the contribution of PP2A to dephosphorylation of my enzyme. I preincubated cells with fostriecin and assayed for enzyme activity.
