EHT 5372

CAT: 0804-HY-111379-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-111379-01Size:5 mg
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AVAILABILITY: InStock
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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, and 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectively[1][2].
CAS Number
[1425945-63-6]
UNSPSC
12352005
Target
CDK; DYRK; GSK-3
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt
Applications
Metabolism-sugar/lipid metabolism
Field of Research
Cancer; Metabolic Disease; Neurological Disease
Assay Protocol
https://www.medchemexpress.com/eht-5372.html
Purity
98.12
Solubility
DMSO : 6.25 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
N=C(C(S1)=NC2=C1C3=C(NC4=CC=C(Cl)C=C4Cl)N=CN=C3C=C2)OC
Molecular Formula
C17H11Cl2N5OS
Molecular Weight
404.27
References & Citations
[1]Séverine Coutadeur, et al. A novel DYRK1A (dual specificity tyrosine phosphorylation-regulated kinase 1A) inhibitor for the treatment of Alzheimer's disease: effect on Tau and amyloid pathologies in vitro. J Neurochem. 2015 May;133 (3) :440-51.|[2]Apirat Chaikuad, et al. An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases. J Med Chem. 2016 Nov 23;59 (22) :10315-10321.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
CLK; DYRK1; DYRK2; DYRK4; GSK-3α; GSK-3β

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