BCI-121

Research use only, not for human use.

BCI-121 (BCI121) is a substrate-competitive SMYD3 inhibitor.

BCI-121 (BCI121) is a substrate-competitive SMYD3 inhibitor that significantly inhibits SMYD3-substrate interaction and chromatin recruitment and is effective in reducing proliferation in various cancer cells types; impairs SMYD3-mediated H4 in vitro methylation, reduced proliferation of HT29 and HCT116 cells; reproduces the effects of SMYD3-targeted RNAi.

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.

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BCI 121 | BCI121

Chromatin/Epigenetic

HMTase

SMYD3

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432529-82-3

340.22

C14H18BrN3O2

>98% (HPLC)

DMSO: 100 mg/mL, 293.93 mM （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=C(NC1=CC=C(Br)C=C1)CN2CCC(C(N)=O)CC2

4-(Aminocarbonyl)-N-(4-bromophenyl)-1-piperidineacetamide

(-20℃)

With Ice Pack

≥ 2 years