EHT 1610

• UNSPSC Description:

  EHT 1610 is a potent inhibitor of DYRK, with IC50s of 0.36 nM (DYRK1A), 0.59 nM (DYRK1B), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cell apoptosis[1]-[4].

• Target Antigen:

  DYRK

• Type:

  Reference compound

• Related Pathways:

  Protein Tyrosine Kinase/RTK

• Applications:

  Neuroscience-Neurodegeneration

• Field of Research:

  Neurological Disease

• Assay Protocol:

  https://www.medchemexpress.com/eht-1610.html

• Purity:

  98.16

• Solubility:

  DMSO : 5 mg/mL (ultrasonic)

• Smiles:

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

• Molecular Weight:

  383.40

• References & Citations:

  [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 Nov 23;59(22):10315-10321.|[2]Thompson B 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[C]// Ash Meeting & Exposition. 2013. l|[3]Bhansali RS, et al. DYRK1A regulates B cell acute lymphoblastic leukemia through phosphorylation of FOXO1 and STAT3. J Clin Invest. 2021 Jan 4;131(1):e135937. |[4]Foucourt A, et al. Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II. Molecules. 2014 Sep 26;19(10):15411-39.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C (Powder, protect from light, stored under nitrogen)

• Clinical Information:

  No Development Reported

• CAS Number:

  1425945-60-3