EHT 5372
Based on 1 Customer Validation
EHT 5372 is a highly potent and selective inhibitor of DYRK's family kinases with IC50s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, and 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectively.
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。
- 純度: 97.38%
- CAS 番号: 1425945-63-6
- 分子式: C17H11Cl2N5OS
- 分子量:404.27
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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DYRK1A 0.22 nM (IC50) |
DYRK1B 0.28 nM (IC50) |
DYRK2 10.8 nM (IC50) |
DYRK4 93.2 nM (IC50) |
CLK1 22.8 nM (IC50) |
CLK2 88.8 nM (IC50) |
CLK4 59.0 nM (IC50) |
GSK-3α 7.44 nM (IC50) |
GSK-3β 221 nM (IC50) |
EHT 5372 (0.1-10 μM; 24 hours) dose-dependently reduces pS396-Tau levels with an IC50 of 1.7 μM whereas cell viability remains over 87% in all conditions[1].
EHT 5372 (0.01-1 μM) inhibits the direct phosphorylation of Tau by DYRK1A[1]
EHT 5372 reduces Aβ production in a dose-dependent reduction with an IC50 of 1.06 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:0.1, 0.5, 1, 5, 10 μM
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Incubation Time:24 hours
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Result:Cell viability remained over 87% in all conditions.
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Cell Line:HEK293 cells
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Concentration:0.01, 0.03, 0.1, 0.3 , 1 μM
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Incubation Time:
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Result:Potently and dose-dependently inhibited Tau phosphorylation at pS396.
化学情報
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CAS 番号 1425945-63-6
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性状 Solid
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分子量 404.27
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分子式 C17H11Cl2N5OS
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Color Off-white to yellow
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SMILES
N=C(C(S1)=NC2=C1C3=C(NC4=CC=C(Cl)C=C4Cl)N=CN=C3C=C2)OC
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 6.25 mg/mL (15.46 mM; ultrasonic and warming and heat to 60°C; 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
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- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Séverine Coutadeur, et al. A novel DYRK1A (dual specificity tyrosine phosphorylation-regulated kinase 1A) inhibitor for the treatment of Alzheimer's disease: effect on Tau and amyloid pathologies in vitro. J Neurochem. 2015 May;133(3):440-51. [Content Brief]
[2]. Apirat Chaikuad, et al. An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases. J Med Chem. 2016 Nov 23;59(22):10315-10321. [Content Brief]
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 | 2.4736 mL | 12.3680 mL | 24.7359 mL | 61.8399 mL |
| 5 mM | 0.4947 mL | 2.4736 mL | 4.9472 mL | 12.3680 mL | |
| 10 mM | 0.2474 mL | 1.2368 mL | 2.4736 mL | 6.1840 mL | |
| 15 mM | 0.1649 mL | 0.8245 mL | 1.6491 mL | 4.1227 mL |
EHT 5372 関連分類
HY-111379 関連分類
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