ER-27319
Based on 1 publication(s) in Google Scholar
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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- Pureza: 98.66%
- No. CAS: 201010-95-9
- Fòrmula: C20H22N2O5
- Peso molecular:370.40
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Immunology/Inflammation Compound Library
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Publications Citing Use of MedChemExpress (MCE) ER-27319
More
Actividad biológica
10 μM (Syk) in human and rat mast cells[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RBL-2H3 | IC50 |
10 μM
Compound: 13, ER-27319
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Inhibition of SYK in rat RBL2H3 cells by immunoprecipitation assay
Inhibition of SYK in rat RBL2H3 cells by immunoprecipitation assay
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[PMID: 22257213] |
| RBL-2H3 | IC50 |
10 μM
Compound: 13, ER-27319
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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
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[PMID: 22257213] |
| RBL-2H3 | IC50 |
10 μM
Compound: 13, ER-27319
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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
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[PMID: 22257213] |
| RBL-2H3 | IC50 |
10 μM
Compound: 13, ER-27319
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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
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[PMID: 22257213] |
| RBL-2H3 | IC50 |
10 μM
Compound: 13, ER-27319
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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
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[PMID: 22257213] |
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.
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Cell Line:RBL-2H3 cells
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Concentration:10, 30 and 100 μM
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Incubation Time:10 min
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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.
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Cell Line:Jurkat cells
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Concentration:3, 10, 30, 100 μM
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Incubation Time:10, 30, 60 min
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Result:IDid not inhibit the the tyrosine phosphorylation of ZAP-70 in response to anti-CD3 stimulation.
Chemical Information
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No. CAS 201010-95-9
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Appearance Solid
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Peso molecular 370.40
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Fòrmula C20H22N2O5
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Color Light yellow to yellow
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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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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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Journal Impact Factor
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Most Recent
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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
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
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 (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.
| 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 |
ER-27319 Related Classifications
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