3MB-PP1 |
| Katalog-Nr.GC14186 |
3MB-PP1, ein voluminÖses Purin-Analogon, ist ein Inhibitor der Polo-Ähnlichen Kinase 1 (Plk1).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 956025-83-5
Sample solution is provided at 25 µL, 10mM.
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3MB-PP1 is a cell-permeable, potent, ATP-competitive, and highly selective inhibitor of polo-like kinase.
Human polo-like kinase 1 (PLK1) plays dominant role in mitosis and the maintenance of genomic stability. PLK1 is overexpressed in human tumours and exihibits prognostic potential in cancer, indicating its involvement in carcinogenesis and its potential as a therapeutic target [2].
In vitro: 3MB-PP1 treatment significantly changed the DNA state. In TbPLKas cells, after treatment with 3MB-PP1 for 9 h, cells at all cell cycle stages showed an increase in detached new flagella when compared with vehicle control-treated samples [1]. The IC50 value of 3MB-PP1 against Ptoas kinase activity was 120 nM. 3MB-PP1 was not able to significantly inhibit Pti1 and MPK2. 3MB-PP1 significantly potentiated the interactions of Ptoas with AvrPto and AvrPtoB1–387[3].
References:
[1] Lozano-Núez A, Ikeda K N, Sauer T, et al. An analogue-sensitive approach identifies basal body rotation and flagellum attachment zone elongation as key functions of PLK in Trypanosoma brucei[J]. Molecular biology of the cell, 2013, 24(9): 1321-1333.
[2] Strebhardt K, Ullrich A. Targeting polo-like kinase 1 for cancer therapy[J]. Nature reviews cancer, 2006, 6(4): 321-330.
[3] Salomon D, Bonshtien A, Mayrose M, et al. Bypassing kinase activity of the tomato Pto resistance protein with small molecule ligands[J]. Journal of Biological Chemistry, 2009, 284(22): 15289-15298.
| Cas No. | 956025-83-5 | SDF | |
| Chemical Name | 1-(1,1-dimethylethyl)-3-[(3-methylphenyl)methyl]-1H-pyrazolo[3,4-d]pyrimidin-4-amine | ||
| Canonical SMILES | NC1=C(C(CC2=CC=CC(C)=C2)=NN3C(C)(C)C)C3=NC=N1 | ||
| Formula | C17H21N5 | M.Wt | 295.4 |
| Löslichkeit | ≤2mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide | Storage | Store at -20°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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3852 mL | 16.9262 mL | 33.8524 mL |
| 5 mM | 0.677 mL | 3.3852 mL | 6.7705 mL |
| 10 mM | 0.3385 mL | 1.6926 mL | 3.3852 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, 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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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