BCI-121 is a substrate-competitive SMYD3 inhibitor that inhibits the proliferation of the cancer cell.

BCI-121显著降低了HT29 (46%)和HCT116 (54%)细胞在72小时内的增殖，并且减少了SMYD3目标基因的表达水平。BCI-121治疗只影响了表达高水平SMYD3的癌细胞系的增殖。在OVCAR-3细胞中检测到的SMYD3高表达水平，以及BCI-121处理后增殖率的显著下降，表明BCI-121对于高SMYD3表达细胞具有特异性的抑制作用。

Cell proliferation is determined using the cell proliferation reagent WST-1. Cells are seeded into 96-well plates one day before treatment. After 48 h, 72 h, or 96 h of BCI-121 or DMSO exposure, 10 μL of the Cell Proliferation Reagent WST-1 are added to each well and incubated at 37 °C in a humidified incubator for up to 1 h. Absorbance is measured on a microplate reader at 450/655 nm. The proliferation index is calculated as the ratio of WST-1 absorbance of treated cells to WST-1 absorbance of control cells.