Art. -Nr.: HY-138961

ER-27319

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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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Reinheit: 98.66%
CAS. Nr.: 201010-95-9
Formel: C₂₀H₂₂N₂O₅
Molecular Weight:370.40

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ER-27319 Chemical Structure

CAS. Nr.: 201010-95-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
RBL-2H3	IC₅₀	10 μM Compound: 13, ER-27319	Inhibition of SYK in rat RBL2H3 cells by immunoprecipitation assay Inhibition of SYK in rat RBL2H3 cells by immunoprecipitation assay	[PMID: 22257213]
RBL-2H3	IC₅₀	10 μM Compound: 13, ER-27319	Inhibition of SYK in rat RBL2H3 cells assessed as reduction in DNP-BSA-stimulated Fcepsilon receptor 1-mediated 5-HT release Inhibition of SYK in rat RBL2H3 cells assessed as reduction in DNP-BSA-stimulated Fcepsilon receptor 1-mediated 5-HT release	[PMID: 22257213]
RBL-2H3	IC₅₀	10 μM Compound: 13, ER-27319	Inhibition of SYK in rat RBL2H3 cells assessed as reduction in DNP-BSA-stimulated Fcepsilon receptor 1-mediated arachidonic acid release Inhibition of SYK in rat RBL2H3 cells assessed as reduction in DNP-BSA-stimulated Fcepsilon receptor 1-mediated arachidonic acid release	[PMID: 22257213]
RBL-2H3	IC₅₀	10 μM Compound: 13, ER-27319	Inhibition of SYK in rat RBL2H3 cells assessed as reduction in DNP-BSA-stimulated Fcepsilon receptor 1-mediated inositol phosphate release Inhibition of SYK in rat RBL2H3 cells assessed as reduction in DNP-BSA-stimulated Fcepsilon receptor 1-mediated inositol phosphate release	[PMID: 22257213]
RBL-2H3	IC₅₀	10 μM Compound: 13, ER-27319	Inhibition of SYK in rat RBL2H3 cells assessed as reduction in DNP-BSA-stimulated Fcepsilon receptor 1-mediated TNFalpha release Inhibition of SYK in rat RBL2H3 cells assessed as reduction in DNP-BSA-stimulated Fcepsilon receptor 1-mediated TNFalpha release	[PMID: 22257213]

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.

Chemical Information

CAS. Nr. 201010-95-9
Appearance Solid
Molecular Weight 370.40
Formel C₂₀H₂₂N₂O₅
Color Light yellow to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (1)

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EMBO Mol Med

Isomeranzin activates Gnas-AMPK signaling to drive white adipose browning and curb obesity in mice. [Abstract]

2025 Nov 26. PMID: 41299101

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (134.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6998 mL

13.4989 mL

26.9978 mL

5 mM

0.5400 mL

2.6998 mL

5.3996 mL

10 mM

0.2700 mL

1.3499 mL

2.6998 mL

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Katsuhiro Moriya, et al. ER-27319, an acridone-related compound, inhibits release of antigen-induced allergic mediators from mast cells by selective inhibition of Fcɛ receptor I-mediated activation of Syk. Proc Natl Acad Sci U S A. 1997 Nov 11; 94(23): 12539–12544.

[2]. Yoshitaka Sato, et al. IgG-mediated signal transduction in canine mastocytoma-derived cells. Int Arch Allergy Immunol. 2002 Dec;129(4):305-13. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6998 mL	13.4989 mL	26.9978 mL	67.4946 mL
	5 mM	0.5400 mL	2.6998 mL	5.3996 mL	13.4989 mL
	10 mM	0.2700 mL	1.3499 mL	2.6998 mL	6.7495 mL
	15 mM	0.1800 mL	0.8999 mL	1.7999 mL	4.4996 mL
	20 mM	0.1350 mL	0.6749 mL	1.3499 mL	3.3747 mL
	25 mM	0.1080 mL	0.5400 mL	1.0799 mL	2.6998 mL
	30 mM	0.0900 mL	0.4500 mL	0.8999 mL	2.2498 mL
	40 mM	0.0675 mL	0.3375 mL	0.6749 mL	1.6874 mL
	50 mM	0.0540 mL	0.2700 mL	0.5400 mL	1.3499 mL
	60 mM	0.0450 mL	0.2250 mL	0.4500 mL	1.1249 mL
	80 mM	0.0337 mL	0.1687 mL	0.3375 mL	0.8437 mL
	100 mM	0.0270 mL	0.1350 mL	0.2700 mL	0.6749 mL

Keywords

ER-27319

1 Cited Publications

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ER-27319

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) ER-27319

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ER-27319

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) ER-27319

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ER-27319 Related Classifications

HY-138961 Related Classifications