[CAS NO. 432529-82-3]  BCI-121

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PRODUCTS SPECIFICATIONS [432529-82-3]

Catalog
HY-21972
Brand
MCE
CAS
432529-82-3

DESCRIPTION [432529-82-3]

Overview

MDLMFCD02149239
Molecular Weight340.22
Molecular FormulaC14H18BrN3O2
SMILESNC(C1CCN(CC(NC2=CC=C(Br)C=C2)=O)CC1)=O

For research use only. We do not sell to patients.


Summary

BCI-121 is a SMYD3 inhibitor that impairs the proliferation of cancer cell.


In Vitro

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 [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 293.93 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9393 mL 14.6964 mL 29.3927 mL
5 mM 0.5879 mL 2.9393 mL 5.8785 mL
10 mM 0.2939 mL 1.4696 mL 2.9393 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.75 mg/mL (8.08 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.75 mg/mL (8.08 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.75 mg/mL (8.08 mM); Clear solution

* All of the co-solvents are available by MCE.