Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
ln Vitro |
BCI-121 efficiently lowers the proliferation of different cancer cell types by substantially inhibiting chromatin recruitment and SMYD3-substrate interaction. After 72 hours, BCI-121 dramatically decreased the HT29 (46% reduction) and HCT116 (54% reduction) cells' ability to proliferate, as well as the expression levels of the SMYD3 target genes. Histone H4 is preferentially methylated by SMYD3, and in vitro SMYD3-mediated H4 methylation is inhibited by BCI-121. Cancer cells treated with BCI-121 had much less growth potential, which accumulated in the S phase of the cell cycle. Targeted methyl marks (H4K5me and H3K4me2) were reduced and cell proliferation was inhibited in a dose-dependent manner in response to BCI-121 treatment. In cancer cell lines overexpressing SMYD3, BCI-121 has antiproliferative characteristics and typically resembles the effects of RNAi targeting SMYD3. BCI-121 inhibits SMYD3 from recruiting to the promoters of its target genes, an event linked to decreased gene expression, according to experiments conducted in cancer cells [1].
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References |
[1]. Peserico A, et al. A SMYD3 Small-Molecule Inhibitor Impairing Cancer Cell Growth. J Cell Physiol. 2015 Oct;230(10):2447-2460
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Molecular Formula |
C14H18BRN3O2
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Molecular Weight |
340.22
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Exact Mass |
339.0582
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CAS # |
432529-82-3
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Related CAS # |
432529-82-3
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SMILES |
O=C(NC1=CC=C(Br)C=C1)CN2CCC(C(N)=O)CC2
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InChi Key |
KSUYPIXCRPCPGF-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C14H18BrN3O2/c15-11-1-3-12(4-2-11)17-13(19)9-18-7-5-10(6-8-18)14(16)20/h1-4,10H,5-9H2,(H2,16,20)(H,17,19)
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Chemical Name |
4-(Aminocarbonyl)-N-(4-bromophenyl)-1-piperidineacetamide
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Synonyms |
BCI-121 BCI 121 BCI121
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~293.93 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (8.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (8.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.75 mg/mL (8.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.