Biochem/physiol Actions
BCI-121 is a substrate-competitive SMYD3 inhibitor that reduces nuclear histone H3 lys4 di- and tri-methylation level (by 50%/H3K4me2 and 40%H3K4me3 in HT29 cells; 100 µM BCI-121 for 48 h), downregulates known SMYD3 target genes transcription, and selectively affects SMYD3-dependent proliferation of cancer cultures (46%/HT29 and 54%/HCT116 proliferation reduction; 100 µM BCI-121 for 72 h) with little antiproliferation efficacy toward low SMYD3-expressing cancer cells. BCI-121 targets SMYD3 via direct affinity interaction (kon 357.7/M/s; koff 4.23×10-3/s; KD=koff/kon = 11.8 µM) and effectively competes against histone for SMYD3 binding (%inhibition/[histone H4 peptide]:[BCI-121] ratio = 36.5%/1:1 and 51.0%/1:2.5).
BCI121 is capable of reducing the mesenchymal signature of MDA-MB-231 cells. It can also decrease their ability to invade in vitroandin vivo.
Packaging
5 mg in glass bottle
| Colour | white to beige |
|---|---|
| Quality Level | 100 |
| Manufacturer | SIGMA-ALDRICH |
| Storage Temp. | 2-8°C |
| Solubility | DMSO: 20 mg/mL, clear |
| Form | powder |
| Assay | ≥98% (HPLC) |
There are no downloads for this product.
