SBE13 Hydrochloride
Based on 1 Customer Validation
SBE13 Hydrochloride is a potent and selective Plk1 inhibitor, with an IC50 of 200 pM; SBE13 Hydrochloride poorly inhibits Plk2 (IC50>66 μM) or Plk3 (IC50=875 nM).
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- Reinheit: 98.56%
- CAS. Nr.: 1052532-15-6
- Formel: C24H28Cl2N2O4
- Molecular Weight:479.40
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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PLK1 200 pM (IC50) |
PLK3 875 nM (IC50) |
SBE13 significantly reduce cell proliferation and induce apoptosis in HeLa cells, with an EC50 of 18 μM[1]. SBE13 (1-100 μM) shows no effect on Caspase 3/7 activity in NIH-3T3 cells. SBE13 (66 and 100 μM) does not change morphology after treatment of primary cells. SBE13 (10 and 100 μM) reduces pRb staining in primary cells, and this indicates a G0/G1 arrest[2]. SBE13 (66 and 100 μM) increases levels of cyclin B1, phospho histone H3, Wee1, Emi1 and securin, and results in cleavage of Cdc27 in HeLa cells. SBE13 (10 and 100 μM) also induces apoptosis of HeLa cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1052532-15-6
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Appearance Solid
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Molecular Weight 479.40
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Formel C24H28Cl2N2O4
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Color Light yellow to yellow
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SMILES
COC1=CC=C(CCNCC2=CC=C(OCC3=CC=C(Cl)N=C3)C(OC)=C2)C=C1OC.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (208.59 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 5 mg/mL (10.43 mM; Need ultrasonic)
* "≥" 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.5 mg/mL (5.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Protokoll
To assay Plk1 kinase activity, cells are lysed after 13 h release in the presence of SBE13 after double thymidine block and kinase is immunoprecipitated from lysates using antibodies. In brief, for each immunoprecipitation 800 μg of total protein are incubated with Plk1 antibody cocktail (1.5 μg) for 2 h at 4°C on a rotator. Immunoprecipitated protein is collected using Protein A/G Agarose beads. Plk1 immunoprecipitates are incubated with casein (1 μg) and with [γ-32P]ATP (1 μCi) for 30 min at 37°C in kinase buffer. Products from the kinase assays are fractionated on 10 % bis-tris-polyacrylamide gels, and phosphorylated substrate is visualized by autoradiography after an exposure of 12-36 h. Equal amounts of immunoprecipitates are subjected to Western blot analysis to confirm equal loading of Plk1 protein in kinase reactions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
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- 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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Handling Instructions (2659 KB)
Verweise
[1]. Keppner S, et al. Identification and validation of a potent type II inhibitor of inactive polo-like kinase 1. ChemMedChem. 2009 Nov;4(11):1806-9. [Content Brief]
[2]. Keppner S, et al. Fate of primary cells at the G?/S boundary after polo-like kinase 1 inhibition by SBE13. Cell Cycle. 2011 Feb 15;10(4):708-20. Epub 2011 Feb 15. [Content Brief]
[3]. Keppner S, et al. Biological impact of freezing Plk1 in its inactive conformation in cancer cells. Cell Cycle. 2010 Feb 15;9(4):761-73. Epub 2010 Feb 16. [Content Brief]
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.0859 mL | 10.4297 mL | 20.8594 mL | 52.1485 mL |
| 5 mM | 0.4172 mL | 2.0859 mL | 4.1719 mL | 10.4297 mL | |
| 10 mM | 0.2086 mL | 1.0430 mL | 2.0859 mL | 5.2149 mL | |
| DMSO | 15 mM | 0.1391 mL | 0.6953 mL | 1.3906 mL | 3.4766 mL |
| 20 mM | 0.1043 mL | 0.5215 mL | 1.0430 mL | 2.6074 mL | |
| 25 mM | 0.0834 mL | 0.4172 mL | 0.8344 mL | 2.0859 mL | |
| 30 mM | 0.0695 mL | 0.3477 mL | 0.6953 mL | 1.7383 mL | |
| 40 mM | 0.0521 mL | 0.2607 mL | 0.5215 mL | 1.3037 mL | |
| 50 mM | 0.0417 mL | 0.2086 mL | 0.4172 mL | 1.0430 mL | |
| 60 mM | 0.0348 mL | 0.1738 mL | 0.3477 mL | 0.8691 mL | |
| 80 mM | 0.0261 mL | 0.1304 mL | 0.2607 mL | 0.6519 mL | |
| 100 mM | 0.0209 mL | 0.1043 mL | 0.2086 mL | 0.5215 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
SBE13 Hydrochloride Related Classifications
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