Harmalol (hydrochloride hydrat

一种β-咔啉生物碱和骆驼蓬碱的活性代谢物；DYRK1A的抑制剂(IC50=0.63µM)；MAO-A的抑制剂(IC50=0.66µM)；对DYRK1A的选择性优于Cdk1、Cdk5、CK1α1、Clk4、DYRK2、Pim-1和GSK3β，但也抑制DYRK1B和Clk1(10µM)；抑制H4人胶质母细胞瘤细胞增殖(IC50s=23.7µM)；降低HepG2细胞中TCDD诱导的CYP1A1水平升高，并防止豚鼠肝细胞浆提取物中TCDD诱导的AhR激活；降低PC12细胞中谷氨酸诱导的细胞毒性、细胞色素c释放、胱天蛋白酶-3激活和ROS生成(25µM)。A β-carboline alkaloid and an active metabolite of harmaline; an inhibitor of DYRK1A (IC50 = 0.63 µM); an inhibitor of MAO-A (IC50 = 0.66 µM); selective for DYRK1A over Cdk1, Cdk5, CK1α1, Clk4, DYRK2, Pim-1, and GSK3β but also inhibits DYRK1B and Clk1 at 10 µM; inhibits proliferation of H4 human glioblastoma cells (IC50s = 23.7 µM); reduces TCDD-induced increases in CYP1A1 levels in HepG2 cells and prevents TCDD-induced activation of AhR in guinea pig hepatic cytosolic extracts; reduces glutamate-induced cytotoxicity, cytochrome c release, caspase-3 activation, and ROS production in PC12 cells at 25 µM.分子式C12H12N2O • HCl [2H2O]分子量272.7OC1=CC=C2C(NC3=C2CCN=C3C)=C1.Cl.O.O