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Harmine

CAS No. : 442-51-3

MCE 国际站：Harmine

产品活性：Harmine 是一种具有抗癌和抗炎活性的天然双特异性酪氨酸磷酸化调节激酶 (DYRK) 抑制剂。Harmine 对 5-HT_2A 血清素受体具有高亲和力，K_i 值为 397 nM。

研究领域：Protein Tyrosine Kinase/RTK  |  Neuronal Signaling  |  GPCR/G Protein

作用靶点：DYRK  |  5-HT Receptor

结构分类：生物碱  |  吲哚类生物碱  |  结构分类

来源：植物  |  蒺藜科  |  骆驼蓬

In Vitro: Harmine inhibits tau phosphorylation by DYRK1A by selected DANDYs, with an IC₅₀ of 190 nM.Harmine negatively regulates homologous recombination (HR) by interfering Rad51 recruitment, resulting in severe cytotoxicity in hepatoma cells. Furthermore, NHEJ inhibitor Nu7441 markedly sensitizes Hep3B cells to the anti-proliferative effects of Harmine.

In Vivo: It is shown that brain water content is significantly increased in the TBI group. Treatment with Harmine significantly reduces the tissue water content at 1, 3 and 5 days, compared with the TBI group. Harmine treatment significantly reduces the escape latency at 3 and 5 days, compared with the TBI group. Post-TBI administration of Harmine significantly improves the motor function recovery of the rats at 1, 3 and 5 days following TBI, compared with the TBI group without Harmine treatment. The neuronal survival rate in the Harmine-treated group is significantly increased, compared with the TBI group. Administration of Harmine results in marked elevation in the expression of GLT-1, compared with the TBI group. The administration of Harmine significantly reduces the expression of caspase 3, compared with the TBI group.

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