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 

Cat. No.: HY-111379 Purity: 95.05%
COA 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, and 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectively.

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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EHT 5372 Related Antibodies

Top Publications Citing Use of Products

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GSK-3 GSK-3α GSK-3β

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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, 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].

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.
Molecular Weight

404.27

Appearance

Solid

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6.67 mg/mL (16.50 mM; ultrasonic and warming and heat to 60°C)

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
10 mM 0.2474 mL 1.2368 mL 2.4736 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation

Purity: ≥98.0%

COA (253 KB) HNMR (122 KB)

Handling Instructions (2659 KB)
References
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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.

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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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