الصفحة الرئيسية>>Signaling Pathways>> Cell Cycle/Checkpoint>> PLK>>3MB-PP1

3MB-PP1

رقم الكتالوجGC14186

3MB-PP1 ، نظير البيورين الضخم ، هو مثبط للكيناز 1 يشبه بولو (Plk1)

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3MB-PP1 التركيب الكيميائي

Cas No.: 956025-83-5

الحجم السعر المخزون الكميّة
1mg
39٫00
متوفر
5mg
94٫00
متوفر
10mM (in 1mL DMSO)
126٫00
متوفر
10mg
149٫00
متوفر
25mg
257٫00
متوفر
50mg
365٫00
متوفر
100mg
512٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of 3MB-PP1

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.

Chemical Properties of 3MB-PP1

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
الذوبان ≤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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of 3MB-PP1

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
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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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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Average Rating: 5 ★★★★★ (Based on Reviews and 33 reference(s) in Google Scholar.)

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