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

EHT 5372 

Cat. No.: HY-111379
Handling Instructions

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, 221 nM for DYRK1A, DYRK1B , DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, GSK-3β.

For research use only. We do not sell to patients.

EHT 5372 Chemical Structure

EHT 5372 Chemical Structure

CAS No. : 1425945-63-6

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Description

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, 221 nM for DYRK1A, DYRK1B , DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, GSK-3β[1][2].

IC50 & Target[1][2]

DYRK1A

0.22 nM (IC50)

DYRK1B

0.28 nM (IC50)

DYRK2

10.8 nM (IC50)

DYRK3

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

404.27

Formula

C₁₇H₁₁Cl₂N₅OS

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

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

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