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)。
| 生物活性 | EHT 1610 is a potent inhibitor ofDYRK, withIC50sof 0.36 nM (DYRK1A), 0.59 nM (DYRK1B), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cellapoptosis[1]-[4]. |
| IC50& Target | IC50: 0.36 nM (DYRK1A), 0.59 nM (DYRK1B)[1] |
体外研究
(In Vitro) | 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: | MHH-CALL-4 cells | | Concentration: | 0, 2.5, 5, 10 μM | | Incubation Time: | 4, 5 hours | | Result: | Reduced p-cyclin D3 (Thr283), and p-FOXO1 protein level in a dose-dependent manner. |
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体内研究
(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: | Xenograft models of B-ALL in mice (12-14 weeks old)[3] | | Dosage: | 20 mg/kg | | Administration: | Intraperitoneal injection; twice a day, 5 days on, 2 days off; 3 weeks | | Result: | Reduced leukemic burden by approximately 8% and conferred a modest survival advantage. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -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。 |
| 溶解性数据 | In Vitro: DMSO : 5 mg/mL(13.04 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.6082 mL | 13.0412 mL | 26.0824 mL | | 5 mM | 0.5216 mL | 2.6082 mL | 5.2165 mL | | 10 mM | 0.2608 mL | 1.3041 mL | 2.6082 mL |
*请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。 |
