BCI-121 |
| Catalog No.: GC18161 |
A substrate-competitive SMYD3 inhibitor?
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
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Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | 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]. |
References: [1]. Peserico A, et al. A SMYD3 Small-Molecule Inhibitor Impairing Cancer Cell Growth. J Cell Physiol. 2015 Oct;230(10):2447-2460. | |
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].
References
[1]. Peserico A, et al. A SMYD3 Small-Molecule Inhibitor Impairing Cancer Cell Growth. J Cell Physiol. 2015 Oct;230(10):2447-2460.
| Cas No. | 432529-82-3 | SDF | |
| Chemical Name | 4-(Aminocarbonyl)-N-(4-bromophenyl)-1-piperidineacetamide | ||
| Canonical SMILES | O=C(NC1=CC=C(Br)C=C1)CN2CCC(C(N)=O)CC2 | ||
| Formula | C14H18BrN3O2 | M.Wt | 340.22 |
| Solubility | Soluble in DMSO | Storage | Store at 2-8°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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