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EHT 1610

Catalog No. T15204   CAS 1425945-60-3
Synonyms: EHT 5372

EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis.

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EHT 1610 Chemical Structure
EHT 1610, CAS 1425945-60-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 147.00
5 mg In stock $ 372.00
10 mg In stock $ 556.00
25 mg In stock $ 896.00
50 mg In stock $ 1,220.00
100 mg In stock $ 1,650.00
500 mg In stock $ 3,290.00
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Purity: 98.27%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis.
Targets&IC50 DYRK2:10.8 nM, CLK1:22.8 nM, DYRK1B:0.28 nM, DYRK1A:0.22 nM, CLK2:88.8 nM, CLK4:59 nM, GSK3α:7.44 nM, DYRK3:93.2 nM, GSK3β:221 nM, DYRK1A :0.36 nM, DYRK1B:0.59 nM
In vitro EHT 1610 triggers apoptosis in primary ALL cells that exhibit resistance to cytarabine treatment.[2]
EHT 1610 demonstrates a dose-dependent induction of apoptosis in B- and T-cell lines as well as primary human pediatric cells.[2]
Treatment with EHT 1610 for a duration of 72 hours leads to the inhibition of DYRK1A, resulting in the disruption of DYRK1A-mediated FOXO1 and STAT3 signaling pathways. This disruption ultimately leads to selective cell death in leukemic B cells.[3]
Exposure to EHT 1610 at concentrations ranging from 2.5 to 10 μM for a period of 4-5 hours results in the inhibition of phosphorylation of FOXO1, STAT3, and cyclin D3. This inhibition leads to the regulation of late cell-cycle progression, mitochondrial ROS levels, and DNA damage, respectively.[3]
In vivo In a murine model of aggressive leukemia, EHT 1610 (20 mg/kg/d; i.p.; twice a day; 3 weeks) demonstrates antileukemia activity when administered intraperitoneally.[3]
Synonyms EHT 5372
Molecular Weight 383.4
Formula C18H14FN5O2S
CAS No. 1425945-60-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.5 mg/mL (11.7 mM), sonification is recommended.

TargetMolReferences and Literature

1. Chaikuad A, 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;59(22):10315-1032 2. Benjamin J, et al. The Chromosome 21 Kinase DYRK1A Controls Cell Cycle Exit and Survival During Lymphoid Development and Is a Novel Therapeutic Target In Acute Lymphoblastic Leukemia. Blood. 2013;21(122): 814. 3. Bhansali RS, et al. DYRK1A regulates B cell acute lymphoblastic leukemia through phosphorylation of FOXO1 and STATJ Clin Invest. 2021;131(1):e135937. 4. Foucourt A, et al. Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II. Molecules. 2014;19(10):15411-15439.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Inhibitor Library Bioactive Compounds Library Max Anti-Obesity Compound Library Antioxidant Compound Library Bioactive Compound Library NF-κB Signaling Compound Library Metabolism Compound Library Anti-Cancer Compound Library

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Keywords

EHT 1610 1425945-60-3 Cell Cycle/Checkpoint NF-Κb PI3K/Akt/mTOR signaling Proteases/Proteasome Stem Cells Tyrosine Kinase/Adaptors GSK-3 NF-κB CDK Tyrosinase DYRK EHT5372 EHT-5372 EHT1610 EHT-1610 EHT 5372 inhibitor inhibit

 

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