2. Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage Stem Cell/Wnt PI3K/Akt/mTOR
  3. DYRK CDK GSK-3
  4. EHT 5372

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.

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EHT 5372

EHT 5372 Estructura química

No. CAS : 1425945-63-6

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EHT 5372 Related Antibodies

Top Publications Citing Use of Products

Ver todos los productos específicos de isoformas DYRK:

Ver todas las isoformas
DYRK1 DYRK2 DYRK3 DYRK4 HIPK PRP4

Ver todos los productos específicos de isoformas CDK:

Ver todas las isoformas
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

Ver todos los productos específicos de isoformas GSK-3:

Ver todas las isoformas
GSK-3 GSK-3α GSK-3β

  • Actividad biológica

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Descripciòn

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[1][2].

IC50 & Target[1][2]

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)

In Vitro

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.

EHT 5372 Related Antibodies

Cell Viability Assay[1]

Cell Line: HEK293 cells
Concentration: 0.1, 0.5, 1, 5, 10 μM
Incubation Time: 24 hours
Result: Cell viability remained over 87% in all conditions.

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 0.01, 0.03, 0.1, 0.3 , 1 μM
Incubation Time:
Result: Potently and dose-dependently inhibited Tau phosphorylation at pS396.
Peso molecular

404.27

Fòrmula

C17H11Cl2N5OS
No. CAS
Appearance

Solid

Color

Off-white to yellow

SMILES

N=C(C(S1)=NC2=C1C3=C(NC4=CC=C(Cl)C=C4Cl)N=CN=C3C=C2)OC
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4736 mL 12.3680 mL 24.7359 mL
5 mM 0.4947 mL 2.4736 mL 4.9472 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Pureza y Documentación

Purity: 98.12%

SDS (251 KB)

COA (253 KB) HNMR (138 KB) RP-HPLC (169 KB) LCMS (385 KB)

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. 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
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EHT 5372 Related Classifications

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:

EHT 53721425945-63-6EHT5372EHT-5372DYRKCDKGSK-3Dual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseCyclin dependent kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3neurodegenerativediseasescancerdiabetesAlzheimerDYRK1ATauamyloidprecursorInhibitorinhibitorinhibit

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Nombre del producto:
EHT 5372
Cat. No.:
HY-111379
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