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

EHT 5372 

Cat. No.: HY-111380
Handling Instructions

EHT 5372 is a strong inhibitor of DYRK’s family kinases, with IC50s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively.

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

EHT 5372 Chemical Structure

EHT 5372 Chemical Structure

CAS No. : 1425945-60-3

Size Stock
250 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

EHT 5372 is a strong inhibitor of DYRK’s family kinases, with IC50s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively.

IC50 & Target

CLK1

22.8 nM (IC50)

Clk2

88.8 nM (IC50)

Clk4

59 nM (IC50)

GSK3α

7.44 nM (IC50)

GSK3β

221 nM (IC50)

DYRK1A

0.22 nM (IC50)

DYRK1B

0.28 nM (IC50)

DYRK2

10.8 nM (IC50)

DYRK3

93.2 nM (IC50)

In Vitro

EHT 5372 is a strong inhibitor of DYRK’s family kinases, with IC50s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively[1][2]. IC50 for DYRK2 and DYRK3 were higher (10.8 and 93.2 nM, respectively) and there was no inhibition on DYRK4. EHT 5372 displayed minimal impact on the CDC2-like kinase (CLK) family, with more than 100x selectivity over CLK1 (CLK1: IC50=22.8 nM; CLK2: IC50=88.8 nM; CLK3: IC50>10 lM; CLK4: no inhibition) and on the glycogen synthase kinase 3 (GSK3) family (GSK3α: IC50=7.44 nM; GSK3β: IC50=221 nM). EHT 5372 inhibits the direct phosphorylation of Tau by DYRK1A. EHT 5372 also normalizes both Aβ-induced Tau phosphorylation and DYRK1A-stimulated Aβ production[2].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6082 mL 13.0412 mL 26.0824 mL
5 mM 0.5216 mL 2.6082 mL 5.2165 mL
10 mM 0.2608 mL 1.3041 mL 2.6082 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

HEK293 cells are changed with new culture medium and treated with 0.1-10 μM DYRK1A inhibitor EHT 5372 or 0.1% DMSO as vehicle for 24 h. The kinase inhibitor is tested in at least three independent experiments performed in duplicate. Cell viability is determined using a standard assay[2].

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

References
Molecular Weight

383.40

Formula

C₁₈H₁₄FN₅O₂S

CAS No.

1425945-60-3

SMILES

N=C(C(S1)=NC2=C1C3=C(NC4=CC=C(OC)C=C4F)N=CN=C3C=C2)OC

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

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

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
EHT 5372
Cat. No.:
HY-111380
Quantity:

EHT 5372

Cat. No.: HY-111380