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Submit ReviewER 27319 maleate is a selective inhibitor of Syk kinase. Inhibits tyrosine phosphorylation of Syk initiated by the engagement of FcεRI in rat and human mast cells. Results in the abrogation of degranulation, TNF-α production (IC50 = 10 μM) and other related signaling events.
ER 27319 maleate is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
M. Wt | 396.17 |
Formula | C18H20N2O.C4H4O4 |
Storage | Desiccate at +4°C |
Purity | ≥99% (HPLC) |
CAS Number | 1204480-26-1 |
PubChem ID | 56972172 |
InChI Key | WVUQPGFRFBVJKH-BTJKTKAUSA-N |
Smiles | OC(=O)\C=C/C(O)=O.CC1=C(C)C2=C(C=C1)C(=O)C1=CC=CC=C1N2CCCN |
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 | |
---|---|---|---|
Solubility | |||
water | 29.71 | 75 | |
DMSO | 39.62 | 100 |
The following data is based on the product molecular weight 396.17. 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 | 2.52 mL | 12.62 mL | 25.24 mL |
5 mM | 0.5 mL | 2.52 mL | 5.05 mL |
10 mM | 0.25 mL | 1.26 mL | 2.52 mL |
50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
References are publications that support the biological activity of the product.
Luskova and Draber (2004) Modulation of the Fcε receptor I signaling by tyrosine kinase inhibitors: search for therapeutic targets of inflammatory and allergy diseases. Curr.Pharm.Des. 10 1727 PMID: 15180535
Moriya et al (1997) ER-27319, an acridone-related compound, inhibits release of antigen-induced allergic mediators from mast cells by selective inhibition of Fce receptor I-mediated activation of Syk. Proc.Natl.Acad.Sci.USA 94 12539
If you know of a relevant reference for ER 27319 maleate, please let us know.
Keywords: ER 27319 maleate, ER 27319 maleate supplier, Selective, Syk, kinases, inhibitors, inhibits, TNF-α, TNF-alpha, production, Interleukins, Tumor, Necrosis, Factor-α, Factor-alpha, Cytokines, ER27319, maleate, Kinase, 2471, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for ER 27319 maleate include:
Rycaj et al (2016) Longitudinal tracking of subpopulation dynamics and molecular changes during LNCaP cell castration and identification of inhibitors that could target the PSA-/lo castration-resistant cells. Oncotarget 7 14220 PMID: 26871947
Ng et al (2008) Receptor-independent, direct membrane binding leads to cell-surface lipid sorting and Syk kinase activation in dendritic cells. Immunity 29 807 PMID: 18993083
Do you know of a great paper that uses ER 27319 maleate from Tocris? Please let us know.
Average Rating: 5 (Based on 1 Review.)
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