2. Protein Tyrosine Kinase/RTK
  3. Syk
  4. 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

ER-27319

ER-27319 構造式

CAS 番号 : 201010-95-9

容量 価格（税別） 在庫状況 数量
5 mg $619 在庫あり
10 mg   お問い合わせ  
50 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Other Forms of ER-27319:

ER-27319 関連抗体

Top Publications Citing Use of Products

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

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]
Cellular Effect
Cell Line Type Value Description References
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 TNFalpha release
Inhibition of SYK in rat RBL2H3 cells assessed as reduction in DNP-BSA-stimulated Fcepsilon receptor 1-mediated TNFalpha 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 by immunoprecipitation assay
Inhibition of SYK in rat RBL2H3 cells by immunoprecipitation assay
[PMID: 22257213]
体外実験

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.

ER-27319 関連抗体

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.
分子量

370.40

分子式

C20H22N2O5
CAS 番号
Appearance

Solid

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

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

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
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 (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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション
参考文献

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

ER-27319 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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-27319201010-95-9ER27319ER 27319SykSpleen tyrosine kinaseRBL-2H3cultured human mast cellshuman peripheral B cellCanine cutaneous mastocytoma-derived cellsInhibitorinhibitorinhibit

最近チェックした製品:

オンラインお問い合わせ

Your information is safe with us. * Required Fields.

製品名

  

カスタマ需要量 *

お名前 *

 

タイトル

メールアドレス *

 

電話番号 *

デパートメント

 

組纖名 *

市区町村

都道府県

国或いは地域 *

      

必ず会社名を記載ください。個人への返信は行いません。

備考

バルクお問い合わせ

Inquiry Information

製品名:
ER-27319
製品番号:
HY-138961
数量:
MCE 日本正規代理店:

カスタマーレビュー

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

製品名

  

Lot #

お名前 *

 

メールアドレス *

電話番号 *

 

部門 *

組纖名 *

 

国或いは地域 *

備考

Request for HNMR Report

We have received your request and will respond to you as soon as possible.