1. Protein Tyrosine Kinase/RTK
  2. Syk
  3. ER-27319

ER-27319, an acridone derivative, is a potent and selective SYK inhibitor, and inhibits the tyrosine phosphorylation of SYK and its activity. ER-27319 inhibits the release of antigen-induced allergic mediators from human and rat mast cells with an IC50 of 10 μM and can be used for study in allergic diseases.

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ER-27319 Chemical Structure

ER-27319 Chemical Structure

CAS No. : 201010-95-9

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Based on 1 publication(s) in Google Scholar

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Description

ER-27319, an acridone derivative, is a potent and selective SYK inhibitor, and inhibits the tyrosine phosphorylation of SYK and its activity. ER-27319 inhibits the release of antigen-induced allergic mediators from human and rat mast cells with an IC50 of 10 μM and can be used for study in allergic diseases[1][2].

IC50 & Target

10 μM (Syk) in human and rat mast cells[1]

In Vitro

ER-27319 (24 h) inhibits antigen-induced generation of inositol phosphates, release of arachidonic acid, and secretion of histamine and tumor necrosis factor α in RBL-2H3 cells, rat peritoneal and human cultured mast cells, and with IC50 value of 10 μM, approximately[1].
ER-27319 (10-30 μM, 10 min) selectivity inhibits the tyrosine phosphorylation of SYK induced by the phosphorylated immunoreceptor tyrosine-based activation motif of the FcεRI γ in RBL-2H3 cells[1].
ER-27319 (up to 100 μM, 60 min) does not inhibit the the tyrosine phosphorylation of ZAP-70 in response to anti-CD3 stimulation in the Jurkat cells[1].
ER-27319 (100 μM, 10 min) inhibits the tyrosine phosphorylation of two proteins (38, 70 kD) and decreases the tyrosine phosphorylation of the other two proteins (62, 80 kD) in anti-IgG stimulation Canine cutaneous mastocytoma-derived cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: RBL-2H3 cells
Concentration: 10, 30 and 100 μM
Incubation Time: 10 min
Result: Inhibited the Tyrosine Phosphorylation of SYK in Mast Cells (the inhibition of 57% and 87% at 10 and 30 μM).
Inhibited the tyrosine phosphorylation of SYK induced by the phospho-γ ITAM of the FcεRI γ but not the tyrosine phosphorylation of Syk induced by the phospho-Ig β immunoreceptor tyrosine-based activation motif at 10 and 30 μM.
Had no effect on the Igβ immunoreceptor tyrosine-based activation motif-induced phosphorylation of SYK at 100 μM.

Western Blot Analysis[1]

Cell Line: Jurkat cells
Concentration: 3, 10, 30, 100 μM
Incubation Time: 10, 30, 60 min
Result: IDid not inhibit the the tyrosine phosphorylation of ZAP-70 in response to anti-CD3 stimulation.
Molecular Weight

370.40

Formula

C20H22N2O5

CAS No.
SMILES

O=C1C2=C(C=CC=C2)N(CCCN)C3=C(C)C(C)=CC=C13.O=C(O)C(O)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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ER-27319 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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ER-27319
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HY-138961
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