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EHT 5372

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Catalog No. T61985Cas No. 1425945-63-6

EHT 5372 is a potent and selective inhibitor of DYRK's family kinases. EHT 5372 shows IC 50 s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, GSK-3β.

EHT 5372

EHT 5372

😃Good
Catalog No. T61985Cas No. 1425945-63-6
EHT 5372 is a potent and selective inhibitor of DYRK's family kinases. EHT 5372 shows IC 50 s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, GSK-3β.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$1,6208-10 weeks8-10 weeks
50 mg$2,1108-10 weeks8-10 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Product Introduction

Bioactivity
Description
EHT 5372 is a potent and selective inhibitor of DYRK's family kinases. EHT 5372 shows IC 50 s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, GSK-3β.
Targets&IC50
DYRK1A:0.22 nM, DYRK4:93.2 nM, DYRK2:10.8 nM, CLK2:88.8 nM, GSK-3α:7.44 nM, GSK-3β:221 nM, DYRK1B:0.28 nM, CLK1:22.8 nM, CLK4:59.0 nM
In vitro
EHT 5372 (0.1-10 μM; 24 hours) dose-dependently reduces pS396-Tau levels with an IC50 of 1.7 μM, maintaining cell viability over 87% in all conditions. It inhibits Tau phosphorylation by DYRK1A (0.01-1 μM) and reduces Aβ production with an IC50 of 1.06 μM. [1]. Cell Line: HEK293 cells. Concentration: 0.1, 0.5, 1, 5, 10 μM; Incubation Time: 24 hours. Results: Cell viability remained over 87%. Concentration: 0.01, 0.03, 0.1, 0.3, 1 μM. Result: Potently inhibited Tau phosphorylation at pS396 dose-dependently.
Chemical Properties
Molecular Weight404.27
FormulaC17H11Cl2N5OS
Cas No.1425945-63-6
SmilesN(C1=C2C3=C(N=C(C(OC)=N)S3)C=CC2=NC=N1)C4=C(Cl)C=C(Cl)C=C4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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