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BCI-121 is an inhibitor of SET and MYND domain-containing protein 3 (SMYD3).1 It inhibits histone H3 lysine 4 (H3K4) di- and trimethylation in HT-29 cell lysates when used at a concentration of 100 µM. BCI-121 (100 µM) inhibits proliferation in a panel of colorectal, lung, pancreatic, prostate, and ovarian cancer cell lines in an SMYD3 expression-dependent manner. It induces cell cycle arrest at the S phase and decreases global H5K4 methylation and H3K4 dimethylation in HT-29 cells in a concentration-dependent manner. Intratumoral injection of BCI-121 (20 µM) reduces tumor volume in an MHCC97H hepatocellular carcinoma (HCC) mouse xenograft model.2
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1. A SMYD3 small-
2. Amplification of SMYD3 promotes tumorigenicity and intrahepatic metastasis of hepatocellular carcinoma via upregulation of CDK2 and MMP2. Oncogene 38(25), 4948-4961 (2019).