BCI-121 |
Catalog No.GC18161
One-Click Copy Product Info
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BCI-121 is a competitive inhibitor of SMYD3, which impairs SMYD3-mediated histone H4 methylation.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 432529-82-3
Sample solution is provided at 25 µL, 10mM.
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BCI-121 is a competitive inhibitor of SMYD3, which impairs SMYD3-mediated histone H4 methylation [1]. BCI-121 competes with histones for binding to SMYD3 and reduces SMYD3 binding to the promoter region of the target genes as well as the expression of downstream effectors ITGB6 and ITGAM[2]. BCI-121 has been widely used to inhibit the proliferation of ovarian cancer cells and the epithelial-mesenchymal transition of breast cancer[3].
In vitro, BCI-121 treatment for 5 days significantly inhibited the proliferation of D458 cells with an IC50 value of 80μM, and led to the downregulation of pRBSer795 and the upregulation of RB protein[4]. Treatment with 100μM BCI-121 for 72 hours significantly inhibited the viability of A549 cells and H1650 cells, and decreased the levels of H3K4me3 and the transcriptional level of ANO1[5]. Treatment with 100μM BCI-121 for 4 days significantly reduced the levels of H4K20me3 and p-Akt (S473) in HGC-27 and SGC-7901 cells, and increased the level of EMP1 protein[6].
In vivo, BCI-121 treatment via daily intraperitoneal injections (1mg/kg) for three consecutive days could reverse the elevated H3K4me3 levels in the tauopathy mouse models, improve the cognitive deficits of the mice and restore the function and expression of neuronal synaptic NMDAR[7]. Three consecutive days of daily intraperitoneal injection of BCI-121 (20mg/kg) exacerbated the renal tubular cell injury and apoptosis induced by ischemia-reperfusion (IR) in mice, resulting in severe renal dysfunction and pathological changes[8].
References:
[1] Peserico A, Germani A, Sanese P, et al. A SMYD3 small‐molecule inhibitor impairing cancer cell growth[J]. Journal of cellular physiology, 2015, 230(10): 2447-2460.
[2] Lyu T, Jiang Y, Jia N, et al. SMYD3 promotes implant metastasis of ovarian cancer via H3K4 trimethylation of integrin promoters[J]. International journal of cancer, 2020, 146(6): 1553-1567.
[3] Rubio-Tomás T. Novel insights into SMYD2 and SMYD3 inhibitors: from potential anti-tumoural therapy to a variety of new applications[J]. Molecular biology reports, 2021, 48(11): 7499-7508.
[4] Asuthkar S, Venkataraman S, Avilala J, et al. SMYD3 promotes cell cycle progression by inducing cyclin D3 transcription and stabilizing the cyclin D1 protein in medulloblastoma[J]. Cancers, 2022, 14(7): 1673.
[5] Zhong D, Zhan Z, Zhang J, et al. SMYD3 regulates the abnormal proliferation of non-small-cell lung cancer cells via the H3K4me3/ANO1 axis: Dian Zhong et al[J]. Journal of biosciences, 2022, 47(3): 53.
[6] Zeng Y, Ma G, Cai F, et al. SMYD3 drives the proliferation in gastric cancer cells via reducing EMP1 expression in an H4K20me3-dependent manner[J]. Cell death & disease, 2023, 14(6): 386.
[7] Williams J B, Cao Q, Wang W, et al. Inhibition of histone methyltransferase Smyd3 rescues NMDAR and cognitive deficits in a tauopathy mouse model[J]. Nature Communications, 2023, 14(1): 91.
[8] Du X, Shen F, Yu C, et al. SMYD3 as an epigenetic regulator of renal tubular cell survival and regeneration following acute kidney injury in mice[J]. The FASEB Journal, 2025, 39(9): e70533.
| Cell experiment [1]: | |
Cell lines | D458 cells |
Preparation Method | D458 cells were grown in DMEM medium with 10% (v/v) fetal bovine serum (FBS), 100U/ml penicillin, and 100μg/ml streptomycin in the presence of 5% CO2 at 37°C. Cells (5×103 cells/ml) were seeded in 96-well plates and allowed to adhere in a 5% CO2 incubator at 37°C overnight. Cells were treated with different concentrations of BCI-121 (0, 10, 20, 40, 80, and 100µM) for 5 days. The cell viability was evaluated. |
Reaction Conditions | 0, 10, 20, 40, 80, and 100µM; 5 days |
Applications | BCI-121 treatment significantly reduced cell viability of D458 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female Balb/c nude mice |
Preparation Method | Female Balb/c nude mice (4-week-old) weighing 20-22g were housed under specific-pathogen-free (SPF) conditions with food and water ad libitum. Mice routinely for one week to adapt to the environment. In total, 2 × 106 SGC-7901 cells were suspended in 100μl of PBS and injected into the dorsal flanks of the mice. For pharmaceutical inhibition experiment, 50μl of BCI-121 (100μM) was administrated intratumorally twice a week after 1 week of incubation. The tumor was collected and weighed at the 18 days after the implantation. The tumor volume was calculated using the following formula: V=(width2×length)×0.5. |
Dosage form | 100μM (50μl); twice a week for 18 days; intratumoral injection |
Applications | BCI-121 treatment significantly reduced the tumor weight and volume in mice with SGC-7901 xenografts. |
References: | |
| 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 | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9393 mL | 14.6964 mL | 29.3927 mL |
| 5 mM | 587.9 μL | 2.9393 mL | 5.8785 mL |
| 10 mM | 293.9 μL | 1.4696 mL | 2.9393 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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.
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Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)