BCL 121;BCI-121;BCI-121;BCI 121;BCI121;BCI-121, 10 mM in DMSO;4-(Aminocarbonyl)-N-(4-bromophenyl)-1-piperidineacetamide;1-Piperidineacetamide, 4-(aminocarbonyl)-N-(4-bromophenyl)-;1-{2-[(4-bromophenyl)amino]-2-oxoethyl}piperidine-4-carboxamide;inhibit,BCI 121,Histone Methyltransferase,Inhibitor,BCI-121,BCI121
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).
