SML1817
BCI-121
≥98% (HPLC)
Sinonimo/i:
4-(Aminocarbonyl)-N-(4-bromophenyl)-1-piperidineacetamide, BCI121
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About This Item
Formula empirica (notazione di Hill):
C14H18BrN3O2
Numero CAS:
Peso molecolare:
340.22
Codice UNSPSC:
12352200
NACRES:
NA.77
Prodotti consigliati
Livello qualitativo
Saggio
≥98% (HPLC)
Forma fisica
powder
Colore
white to beige
Solubilità
DMSO: 20 mg/mL, clear
Temperatura di conservazione
2-8°C
Azioni biochim/fisiol
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.
Codice della classe di stoccaggio
11 - Combustible Solids
Classe di pericolosità dell'acqua (WGK)
WGK 3
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Protein methylation is one of the important post-translational modifications. Although its biological and physiological functions were unknown for a long time, we and others have characterized a number of protein methyltransferases, which have unveiled the critical functions of protein methylation
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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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