BCI-121

SMYD3抑制剂；浓度为100µM时可抑制HT-29细胞裂解物中的H3K4二甲基化和三甲基化；以SMYD3表达依赖性方式抑制结直肠癌、肺癌、胰腺癌、前列腺癌和卵巢癌细胞系中的增殖；诱导细胞周期停滞在S期并降低HT-29细胞中的整体H5K4甲基化和H3K4二甲基化；20µM时肿瘤内注射可减小MHCC97H HCC小鼠异种移植模型中的肿瘤体积。An inhibitor of SMYD3; inhibits H3K4 di- and trimethylation in HT-29 cell lysates at 100 µM; inhibits proliferation in a panel of colorectal, lung, pancreatic, prostate, and ovarian cancer cell lines in an SMYD3 expression-dependent manner; induces cell cycle arrest at the S phase and decreases global H5K4 methylation and H3K4 dimethylation in HT-29 cells; intratumoral injection reduces tumor volume in an MHCC97H HCC mouse xenograft model at 20 µM.分子式C14H18BrN3O2分子量340.2O=C(C1CCN(CC1)CC(NC2=CC=C(C=C2)Br)=O)N