432529-82-3
432529-82-3 structure
- Name: BCI-121
- Chemical Name: BCI-121
- CAS Number: 432529-82-3
- Molecular Formula: C14H18BrN3O2
- Molecular Weight: 340.216
- Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
- Create Date: 2018-02-19 18:48:28
- Modify Date: 2024-01-03 10:54:13
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BCI-121 is a SMYD3 inhibitor that impairs the proliferation of cancer cell.
| Name | BCI-121 |
|---|---|
| Synonyms |
1-Piperidineacetamide, 4-(aminocarbonyl)-N-(4-bromophenyl)-
1-{2-[(4-Bromophenyl)amino]-2-oxoethyl}-4-piperidinecarboxamide |
| Description | BCI-121 is a SMYD3 inhibitor that impairs the proliferation of cancer cell. |
|---|---|
| Related Catalog | |
| In Vitro | 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[1]. |
| Cell Assay | 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[1]. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 576.1±50.0 °C at 760 mmHg |
| Molecular Formula | C14H18BrN3O2 |
| Molecular Weight | 340.216 |
| Flash Point | 302.2±30.1 °C |
| Exact Mass | 339.058228 |
| LogP | 1.80 |
| Vapour Pressure | 0.0±1.6 mmHg at 25°C |
| Index of Refraction | 1.619 |
| Storage condition | 2-8℃ |