EHT 1610 是双特异性酪氨酸磷酸化调节酶 (DYRK) 的强效抑制剂，抑制 DYRK1A 和 DYRK1B 的 IC₅₀ 分别为 0.36 nM 和 0.59 nM。EHT 1610 具有抗白血病的作用，并能够调节细胞周期，诱导细胞凋亡 (apoptosis)。

EHT 1610 is a potent inhibitor of DYRK, with IC 50 s of 0.36 nM (DYRK1A), 0.59 nM (DYRK1B), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cell apoptosis.

Solid

IC50: 0.36 nM (DYRK1A), 0.59 nM (DYRK1B)

EHT 1610 induces apoptosis of primary ALL cells that were resistant to cytarabine.
EHT 1610 dose-dependently induces apoptosis in B- and T-cell lines and primary human pediatric.
EHT 1610 (; 72 h) inhibits DYRK1A, results loss of DYRK1A-mediated FOXO1 and STAT3 signaling, leading to preferential cell death in leukemic B cells.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.

EHT 1610 (20 mg/kg/d; i.p.; twice a day; 3 weeks) shows antileukemia activity against in leukemic aggressive model in mice.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Xenogra

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[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

In Vitro: DMSO : 5 mg/mL (13.04 mM; Need ultrasonic)配制储备液