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3MB-PP1
polo-like kinase 1 (Plk1) allele inhibitor,ATP-competitive

Catalog No.C3340
Size Price Stock Qty
5mg
$103.00
In stock
10mg
$191.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

3MB-PP1

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Chemical Properties

Cas No. 956025-83-5 SDF Download 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
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
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.

Background

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.