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.

Product information

CAS Number: 1425945-63-6

Molecular Weight: 404.27

Formula: C17H11Cl2N5OS

Chemical Name: methyl 9-[(2,4-dichlorophenyl)amino]-[1,3]thiazolo[5,4-f]quinazoline-2-carboximidate

Smiles: COC(=N)C1=NC2=CC=C3N=CN=C(NC4=CC=C(Cl)C=C4Cl)C3=C2S1

InChiKey: QSGKPYRFWJINEH-UHFFFAOYSA-N

InChi: InChI=1S/C17H11Cl2N5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. EHT 5372 (0.01-1 μM) inhibits the direct phosphorylation of Tau by DYRK1A EHT 5372 reduces Aβ production in a dose-dependent reduction with an IC50 of 1.06 μM.

Products are for research use only. Not for human use.