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Fostriecin sodium salt
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.
|Storage||Desiccate at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 452.37. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.21 mL||11.05 mL||22.11 mL|
|5 mM||0.44 mL||2.21 mL||4.42 mL|
|10 mM||0.22 mL||1.11 mL||2.21 mL|
|50 mM||0.04 mL||0.22 mL||0.44 mL|
References are publications that support the biological activity of the product.
Tunac et al (1983) Novel antitumor agents CI-920, PD 113,270 and PD 113,271. I. Taxonomy, fermentation and biological properties. J.Antibiot. 36 1595 PMID: 6689323
Walsh et al (1997) Fostriecin, an antitumor antibiotic with inhibitory activity against serine/threonine protein phosphatases types 1 (PP1) and 2A (PP2A), is highly selective for PP2A. FEBS Lett. 416 230 PMID: 9373158
Hastie and Cohen (1998) Purification of protein phosphatase 4 catalytic subunit: inhibition by the antitumour drug fostriecin and other tumour suppressors and promoters. FEBS Lett. 431 357 PMID: 9714542
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Keywords: Fostriecin sodium salt, Fostriecin sodium salt supplier, Potent, PP2A, PP4, inhibitors, inhibits, Calcineurin, Protein, Ser/Thr, protein, phosphatases, 2A, 4, antibiotics, Phosphatases, Antibiotics, 1840, Tocris Bioscience
7 Citations for Fostriecin sodium salt
Citations are publications that use Tocris products. Selected citations for Fostriecin sodium salt include:
Xu et al (2010) Amphetamine modulation of long-term potentiation in the prefrontal cortex: dose dependency, monoaminergic contributions, and paradoxical rescue in hyperDArgic mutant. J Neurosci 115 1643 PMID: 20969573
Goffin et al (2010) DA-dependent tuning of striatal inhibitory synaptogenesis. J Neurosci 30 2935 PMID: 20181591
Chiu et al (2019) NMDAR-Activated PP1 Dephosphorylates GluN2B to Modulate NMDAR Synaptic Content. Cell Rep 28 332 PMID: 31291571
Xu et al (2009) HyperDArgic tone erodes prefrontal long-term potential via a D2 receptor-operated protein phosphatase gate. J Neurosci 29 14086 PMID: 19906957
Liu (2018) In vivo brain GPCR signaling elucidated by phosphoproteomics. Science 360 eaao4927 PMID: 29930108
Pribiag and Stellwagen (2013) TNF-α Downregulates Inhibitory Neurotransmission through Protein Phosphatase 1-Dependent Trafficking of GABAA Receptors. J Neurosci 33 15879 PMID: 24089494
Chen et al (2014) 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 J Neurosci 34 9621 PMID: 25031403
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Reviews for Fostriecin sodium salt
Average Rating: 4.3 (Based on 3 Reviews.)
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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.
Literature in this Area
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