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
Biological ActivityPotent 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Novel antitumor agents CI-920, PD 113,270 and PD 113,271. I. Taxonomy, fermentation and biological properties.
Tunac et al.
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
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
NMDAR-Activated PP1 Dephosphorylates GluN2B to Modulate NMDAR Synaptic Content.
Authors: Chiu Et al.
Cell Rep 2019;28:332
In vivo brain GPCR signaling elucidated by phosphoproteomics.
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
TNF-α Downregulates Inhibitory Neurotransmission through Protein Phosphatase 1-Dependent Trafficking of GABAA Receptors.
Authors: Pribiag and Stellwagen
J Neurosci 2013;33:15879
DA-dependent tuning of striatal inhibitory synaptogenesis.
Authors: Goffin Et al.
J Neurosci 2010;30:2935
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
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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Reviews for Fostriecin sodium salt
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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.