1. Epigenetics
  2. Histone Methyltransferase
  3. BCI-121

BCI-121 

Cat. No.: HY-21972 Purity: 99.45%
Handling Instructions

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

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

BCI-121 Chemical Structure

BCI-121 Chemical Structure

CAS No. : 432529-82-3

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
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10 mg USD 114 In-stock
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25 mg USD 234 In-stock
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50 mg USD 408 In-stock
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100 mg USD 708 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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].

Molecular Weight

340.22

Formula

C₁₄H₁₈BrN₃O₂

CAS No.

432529-82-3

SMILES

NC(C1CCN(CC(NC2=CC=C(Br)C=C2)=O)CC1)=O

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 provided by MCE.
References
Cell Assay
[1]

Cell proliferation is determined using the cell proliferation reagent WST-1. Cells are seeded into 96-well plates one day before treatment. After 48 h, 72 h, or 96 h of BCI-121 or DMSO exposure, 10 μL of the Cell Proliferation Reagent WST-1 are added to each well and incubated at 37 °C in a humidified incubator for up to 1 h. Absorbance is measured on a microplate reader at 450/655 nm. The proliferation index is calculated as the ratio of WST-1 absorbance of treated cells to WST-1 absorbance of control cells[1].

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

References

Purity: 99.45%

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Keywords:

BCI-121BCI121BCI 121Histone MethyltransferaseInhibitorinhibitorinhibit

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Product Name:
BCI-121
Cat. No.:
HY-21972
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