2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
BCI-121 significantly inhibits SMYD3-substrate interaction and chromatin recruitment and is effective in reducing proliferation in various cancer cells types. BCI-121 significantly reduces proliferation of HT29 (by 46%) and HCT116 (by 54%) cells at 72 h and decreases the expression levels of SMYD3 target genes. SMYD3 preferentially methylates histone H4, and the presence of BCI-121 impairs SMYD3-mediated H4 in vitro methylation. Cancer cells treated with BCI-121 show a significant reduction in their growth ability and accumulated in the S phase of the cell cycle. Cells treated with BCI-121 shows a dose-dependent relationship between SMYD3 impairment and both inhibition of proliferation and reduction of targeted methyl marks (H4K5me and H3K4me2). BCI-121 shows antiproliferative properties in cancer cell lines overexpressing SMYD3 and, in general, replicated the effects of SMYD3-targeted RNAi. Experiments performed in cancer cells show that BCI-121 prevents SMYD3 recruitment on the promoters of its target genes and this event is correlated with reduced gene expression.
