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

ER-27319 (maleate), an acridone derivative, is a potent and selective SKY inhibitor, and inhibits the tyrosine phosphorylation of SYK and its activity. ER-27319 (maleate) 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] .

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ER-27319 maleate Chemical Structure

ER-27319 maleate Chemical Structure

CAS No. : 1204480-26-1

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Based on 1 publication(s) in Google Scholar

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ER-27319 maleate Related Antibodies

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Description

ER-27319 (maleate), an acridone derivative, is a potent and selective SKY inhibitor, and inhibits the tyrosine phosphorylation of SYK and its activity. ER-27319 (maleate) 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 (maleate) (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 (maleate) (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 (maleate) (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 (maleate) (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.

ER-27319 maleate Related Antibodies

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: Did not inhibit the the tyrosine phosphorylation of ZAP-70 in response to anti-CD3 stimulation.
Molecular Weight

396.44

Formula

C22H24N2O5
CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (315.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5224 mL 12.6122 mL 25.2245 mL
5 mM 0.5045 mL 2.5224 mL 5.0449 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: ≥99.4%

COA (253 KB) Elemental Analysis Report (111 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5224 mL 12.6122 mL 25.2245 mL 63.0612 mL
5 mM 0.5045 mL 2.5224 mL 5.0449 mL 12.6122 mL
10 mM 0.2522 mL 1.2612 mL 2.5224 mL 6.3061 mL
15 mM 0.1682 mL 0.8408 mL 1.6816 mL 4.2041 mL
20 mM 0.1261 mL 0.6306 mL 1.2612 mL 3.1531 mL
25 mM 0.1009 mL 0.5045 mL 1.0090 mL 2.5224 mL
30 mM 0.0841 mL 0.4204 mL 0.8408 mL 2.1020 mL
40 mM 0.0631 mL 0.3153 mL 0.6306 mL 1.5765 mL
50 mM 0.0504 mL 0.2522 mL 0.5045 mL 1.2612 mL
60 mM 0.0420 mL 0.2102 mL 0.4204 mL 1.0510 mL
80 mM 0.0315 mL 0.1577 mL 0.3153 mL 0.7883 mL
100 mM 0.0252 mL 0.1261 mL 0.2522 mL 0.6306 mL
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ER-27319 maleate Related Classifications

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.

Keywords:

ER-273191204480-26-1ER27319ER 27319SykSpleen tyrosine kinaseRBL-2H3cultured human mast cellshuman peripheral B cellCanine cutaneous mastocytoma-derived cellsInhibitorinhibitorinhibit

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