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Submit ReviewFostriecin 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.
分子量 | 452.37 |
公式 | C19H26O9PNa |
储存 | Desiccate at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 87860-39-7 |
PubChem ID | 16759606 |
InChI Key | XBUIKNRVGYFSHL-IAVQPKKASA-M |
Smiles | [Na+].C[C@@](O)(\C=C\[C@H]1CC=CC(=O)O1)[C@@H](C[C@@H](O)\C=C/C=C\C=C\CO)OP(O)([O-])=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
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
关键词: 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
引用文献是使用了 Tocris 产品的出版物。 Fostriecin sodium salt 的部分引用包括:
Chiu et al (2019) NMDAR-Activated PP1 Dephosphorylates GluN2B to Modulate NMDAR Synaptic Content. Cell Rep 28 332 PMID: 31291571
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
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
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
Pribiag and Stellwagen (2013) TNF-α Downregulates Inhibitory Neurotransmission through Protein Phosphatase 1-Dependent Trafficking of GABAA Receptors. J Neurosci 33 15879 PMID: 24089494
Liu (2018) In vivo brain GPCR signaling elucidated by phosphoproteomics. Science 360 eaao4927 PMID: 29930108
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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.