EHT 1610
作者：齐岳
发布时间：2023-09-13
16:59:50
点击数：
产品名称：EHT 1610
产品描述：
| 产品描述 | EHT 1610 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. |
| 靶点活性 | DYRK2:10.8 nM, CLK2:88.8 nM, DYRK1B:0.28 nM, CLK1:22.8 nM, GSK3β:221 nM, DYRK3:93.2 nM, GSK3α:7.44 nM, DYRK1B:0.59 nM, DYRK1A :0.36 nM, CLK4:59 nM, DYRK1A:0.22 nM |
| 体外活性 | 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] |
| 体内活性 | 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] |
| 别名 | EHT 5372 |
| 分子量 | 383.4 |
| 分子式 | C18H14FN5O2S |
| CAS No. | 1425945-60-3 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 4.5 mg/mL (11.7 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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