| Bioactivity | 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 | IC50: 0.36 nM (DYRK1A), 0.59 nM (DYRK1B) |
| Invitro | EHT 1610 induces apoptosis of primary ALL cells that were resistant to cytarabine[2].EHT 1610 dose-dependently induces apoptosis in B- and T-cell lines and primary human pediatric[2].EHT 1610 (; 72 h) inhibits DYRK1A, results loss of DYRK1A-mediated FOXO1 and STAT3 signaling, leading to preferential cell death in leukemic B cells[3].EHT 1610 (2.5-10 μM; 4-5 h) inhibits phosphorylation of FOXO1, STAT3 and cyclin D3, thus regulates late cell-cycle progression, mitochondrial ROS and DNA damage, respectively[3]. Western Blot Analysis[3] Cell Line: |
| In Vivo | EHT 1610 (20 mg/kg/d; i.p.; twice a day; 3 weeks) shows antileukemia activity against in leukemic aggressive model in mice[3]. Animal Model: |
| Name | EHT 1610 |
| CAS | 1425945-60-3 |
| Formula | C18H14FN5O2S |
| Molar Mass | 383.40 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, protect from light, stored under nitrogen *该产品在溶液状态不稳定，建议您现用现配，即刻使用。 |
| Reference | [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): [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. |
EHT 1610
CAS: 1425945-60-3 F: C18H14FN5O2S W: 383.40
EHT 1610 is a potent inhibitor of DYRK, with IC50s of 0.36 nM (DYRK1A), 0.59 nM (DYRK1B), respectively. EHT 1610 exhibit
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