MS023

型PRMT抑制剂（对于PRMT1、-3、-4、-6和-8，IC50分别为30、119、83、4和5nM）；10µM时，对I型PRMT的选择性优于PRMT5、-7和-9，以及一组25种PKMT和DNMT；抑制MCF-7细胞中的H4R3甲基化和HEK293细胞中的H3R2甲基化（IC50分别为9和56nM）；20µM时，抑制SARS-CoV-2核衣壳蛋白的甲基化和Vero E6细胞中SARS-CoV-2的复制；160mg/kg时，降低Huh7小鼠异种移植模型中的肿瘤生长。An inhibitor of type I PRMTs (IC50s = 30, 119, 83, 4, and 5 nM for PRMT1, -3, -4, -6, and -8, respectively); selective for these type I PRMTs over PRMT5, -7, and -9, as well as a panel of 25 PKMTs and DNMTs at 10 µM; inhibits methylation of H4R3 in MCF-7 cells and H3R2 in HEK293 cells (IC50s = 9 and 56 nM, respectively); inhibits methylation of the SARS-CoV-2 nucleocapsid protein and the replication of SARS-CoV-2 in Vero E6 cells at 20 µM; reduces tumor growth in a Huh7 mouse xenograft model at 160 mg/kg.分子式C17H25N3O分子量287.4CC(C)OC1=CC=C(C2=CNC=C2CN(C)CCN)C=C1