SML1817
BCI-121
≥98% (HPLC)
Sinónimos:
4-(Aminocarbonyl)-N-(4-bromophenyl)-1-piperidineacetamide, BCI121
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About This Item
Fórmula empírica (notación de Hill):
C14H18BrN3O2
Número de CAS:
Peso molecular:
340.22
UNSPSC Code:
12352200
NACRES:
NA.77
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Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
2-8°C
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 vitro and in vivo.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
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Cancer science, 107(4), 377-384 (2016-01-12)
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Alessia Peserico et al.
Journal of cellular physiology, 230(10), 2447-2460 (2015-03-03)
SMYD3 is a histone lysine methyltransferase that plays an important role in transcriptional activation as a member of an RNA polymerase complex, and its oncogenic role has been described in different cancer types. We studied the expression and activity of
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