SBE 13 HClInactive Plk1 inhibitor CAS# 1052532-15-6 |
Quality Control & MSDS
3D structure
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| Cas No. | 1052532-15-6 | SDF | Download SDF |
| PubChem ID | 11948807 | Appearance | Powder |
| Formula | C24H28Cl2N2O4 | M.Wt | 479.4 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 100 mg/mL (208.59 mM) H2O : 5 mg/mL (10.43 mM; Need ultrasonic) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | N-[[4-[(6-chloropyridin-3-yl)methoxy]-3-methoxyphenyl]methyl]-2-(3,4-dimethoxyphenyl)ethanamine;hydrochloride | ||
| SMILES | COC1=C(C=C(C=C1)CCNCC2=CC(=C(C=C2)OCC3=CN=C(C=C3)Cl)OC)OC.Cl | ||
| Standard InChIKey | QBGSVDJLQQXEGG-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C24H27ClN2O4.ClH/c1-28-20-7-4-17(12-22(20)29-2)10-11-26-14-18-5-8-21(23(13-18)30-3)31-16-19-6-9-24(25)27-15-19;/h4-9,12-13,15,26H,10-11,14,16H2,1-3H3;1H | ||
| 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. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Selective inhibitor of PLK1 (IC50 values are 200 pM, 875 nM and 66 μM for PLK1, PLK3 and PLK2 respectively). Exhibits no effect on Aurora kinase A activity. Binds and stabilizes the inactive form of PLK1. Delays cell cycle progression, reduces cell proliferation and induces apoptosis in a range of human cancer cell lines. Transiently arrests cells cycle at G0/G1 in primary cells. |
SBE 13 HCl Dilution Calculator
SBE 13 HCl Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.0859 mL | 10.4297 mL | 20.8594 mL | 41.7188 mL | 52.1485 mL |
| 5 mM | 0.4172 mL | 2.0859 mL | 4.1719 mL | 8.3438 mL | 10.4297 mL |
| 10 mM | 0.2086 mL | 1.043 mL | 2.0859 mL | 4.1719 mL | 5.2149 mL |
| 50 mM | 0.0417 mL | 0.2086 mL | 0.4172 mL | 0.8344 mL | 1.043 mL |
| 100 mM | 0.0209 mL | 0.1043 mL | 0.2086 mL | 0.4172 mL | 0.5215 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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The serine/threonine kinase polo-like kinase 1 (Plk1) attracts great attention in the field of cancer therapy because it exhibits generally elevated activity in cancer cells and is a negative prognostic factor for cancer patients. The importance of Plk1 activity as a measure for the aggressiveness of a tumor results from its important role in mitotic checkpoints. SBE13 is identified as a novel and potent inhibitor of inactive Plk1.
In vitro: To determine its ability to induce cell death in cancer cells, we applied kinase assays, western blot analyses, FACS can analyses, Caspase assays and immunofluorescence studies. We detected decreased cell proliferation, delayed progression through the cell cycle in lower SBE13 concentrations, a G2/M arrest using higher SBE13 concentrations followed by apoptosis, and abnormal mitotic figures. Notably, SBE13 did not influence activity of other kinases (Plk2, Plk3, Aurora A), indicating the selectivity of this type II Plk1 inhibitor [1].
In silico: The docking pose of SBE13 in the homology model suggests an interaction with Arg 95 of Plk1, and thus spans the whole hydrophobic pocket, which is anticipated for a type II inhibitor. Another SBE13’s characteristic feature of type II inhibitors is the interaction with the hinge region and with the Asp in the Asp-Phe-Gly (DFG) motif [2].
Clinical trial: Up to now, SBE13 is still in the preclinical development stage.
Reference:
[1] Keppner S, Proschak E, Kaufmann M, Strebhardt K, Schneider G, Sp?nkuch B. Biological impact of freezing Plk1 in its inactive conformation in cancer cells. Cell Cycle. 2010 Feb 15;9(4):761-73.
[2] Keppner S, Proschak E, Schneider G, Sp?nkuch B. Identification and validation of a potent type II inhibitor of inactive polo-like kinase 1. ChemMedChem. 2009 Nov;4(11):1806-9.
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Fate of primary cells at the G(1)/S boundary after polo-like kinase 1 inhibition by SBE13.[Pubmed:21301227]
Cell Cycle. 2011 Feb 15;10(4):708-20.
Human polo-like kinase 1 (Plk1), a key regulator of mitosis, is over-expressed in various human tumors. It is a negative prognostic factor for cancer patients and a measure for the aggressiveness of a tumor. Thus, targeting Plk1 might be a promising approach for cancer therapy. Plk1 inhibitors represent attractive tools for cancer research and for the mechanistic investigation of checkpoint control. Here, we show the impact of Plk1 inhibition on cell cycle regulation in primary cells. After treatment with SBE13 the G(1)//S checkpoint was intact, indicated by reduced pRb, resulting in slower cell cycle progression but overall cell proliferation was not significantly impaired. Thus, we provide strong evidence that SBE13 leaves checkpoint control in primary cells unaffected making it a remarkable future anti-cancer therapeutic.
Biological impact of freezing Plk1 in its inactive conformation in cancer cells.[Pubmed:20139717]
Cell Cycle. 2010 Feb 15;9(4):761-73.
Human polo-like kinase 1 (Plk1), a key regulator of mitosis, is overexpressed in various human tumors. It is a negative prognostic factor for cancer patients and a measure for the aggressiveness of a tumor. Thus, targeting Plk1 might be a promising approach for cancer therapy. Kinase inhibitors are divided in type I inhibitors, targeting the highly conserved active conformation, and the more selective type II inhibitors, targeting the inactive conformation of kinases. We analyzed our previously identified type II Plk1 inhibitor SBE13 which is able to inhibit Plk1 activity. To determine its ability to induce cell death in cancer cells, we applied kinase assays, western blot analyses, FACScan analyses, Caspase assays and immunofluorescence studies. We detected decreased cell proliferation, delayed progression through the cell cycle in lower SBE13 concentrations, a G(2)/M arrest using higher SBE13 concentrations followed by apoptosis, and abnormal mitotic figures. Notably, SBE13 did not influence activity of other kinases (Plk2, Plk3, Aurora A), indicating the selectivity of this type II Plk1 inhibitor. This study suggests that Plk1 kinase inhibitors targeting the inactive conformation of Plk1 may be considered for the development of cancer therapeutics.
