BCI-121
Based on 5 publication(s) in Google Scholar
BCI-121 is a SMYD3 inhibitor that impairs the proliferation of cancer cell.
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- Pureté: 99.89%
- CAS No.: 432529-82-3
- Formule: C14H18BrN3O2
- Masse moléculaire:340.22
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) BCI-121
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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In Vivo Efficacy Study
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IHC
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Histological Imaging/Staining
Voir tous les produits spécifiques à Isoform Histone Methyltransferase
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Activité biologique
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SMYD3 |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 432529-82-3
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Appearance Solid
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Masse moléculaire 340.22
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Formule C14H18BrN3O2
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Color Light yellow to yellow
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SMILES
NC(C1CCN(CC(NC2=CC=C(Br)C=C2)=O)CC1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
SMYD3 drives the proliferation in gastric cancer cells via reducing EMP1 expression in an H4K20me3-dependent manner. [Abstract]2023 Jun 29;14(6):386. PMID: 37386026
BCI-121 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jun 29;14(6):386. [Abstract]
SMYD3 inhibitor BCI-121 (100 μM) substantially mitigated the cellular proliferation of HGC-27 and SGC-7901 cells within the indicated time interval by CCK-8 assay.
BCI-121 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jun 29;14(6):386. [Abstract]
BCI-121 (100 μM) remarkably reduced the level of H4K20me3 and p-Akt (S473), as well as increased EMP1 protein level in HGC-27 and SGC-7901 cells by immunoblot assay.
BCI-121 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jun 29;14(6):386. [Abstract]
Tumor growth curves and tumor weight shows that BCI-121 (100 μM) markedly repressed the growth of SGC-7901 cells in vivo.
BCI-121 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jun 29;14(6):386. [Abstract]
IHC shows that Ki-67 staining was markedly weaker in tumor masses originated from BCI-121 (100 μM)-treated mice.
BCI-121 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jun 29;14(6):386. [Abstract]
Administration of BCI-121 in vivo did not elicit evident damages to the livers and kidneys of the BCI-121 (100 μM)-treated mice by HE staining assay.
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Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
Oncogene
2021 Apr;40(15):2711-2724. PMID: 33712705 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
iScience
SMYD3 induces sorafenib resistance by activating SMAD2/3-mediated epithelial-mesenchymal transition in hepatocellular carcinoma. [Abstract]2023 May 29;26(7):106994. PMID: 37534166
Solvant et solubilité
DMSO : ≥ 100 mg/mL (293.93 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9393 mL | 14.6964 mL | 29.3927 mL | 73.4819 mL |
| 5 mM | 0.5879 mL | 2.9393 mL | 5.8785 mL | 14.6964 mL | |
| 10 mM | 0.2939 mL | 1.4696 mL | 2.9393 mL | 7.3482 mL | |
| 15 mM | 0.1960 mL | 0.9798 mL | 1.9595 mL | 4.8988 mL | |
| 20 mM | 0.1470 mL | 0.7348 mL | 1.4696 mL | 3.6741 mL | |
| 25 mM | 0.1176 mL | 0.5879 mL | 1.1757 mL | 2.9393 mL | |
| 30 mM | 0.0980 mL | 0.4899 mL | 0.9798 mL | 2.4494 mL | |
| 40 mM | 0.0735 mL | 0.3674 mL | 0.7348 mL | 1.8370 mL | |
| 50 mM | 0.0588 mL | 0.2939 mL | 0.5879 mL | 1.4696 mL | |
| 60 mM | 0.0490 mL | 0.2449 mL | 0.4899 mL | 1.2247 mL | |
| 80 mM | 0.0367 mL | 0.1837 mL | 0.3674 mL | 0.9185 mL | |
| 100 mM | 0.0294 mL | 0.1470 mL | 0.2939 mL | 0.7348 mL |
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