BCI-121

BCI-121

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

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Code Description Colour Quality Level Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575421 BCI-121 white to beige 100 SIGMA-ALDRICH 2-8°C
£536.25 (exc VAT) per 25MG
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3575422 BCI-121 white to beige 100 SIGMA-ALDRICH 2-8°C
£165.75 (exc VAT) per 5MG
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