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3MB-PP1
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
3MB-PP1图片
CAS NO:956025-83-5
包装与价格：
包装价格(元)
5mg电议
10mg电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt295.4
Cas No.956025-83-5
FormulaC17H21N5
Solubility≤2mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide
Chemical Name1-(1,1-dimethylethyl)-3-[(3-methylphenyl)methyl]-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Canonical SMILESNC1=C(C(CC2=CC=CC(C)=C2)=NN3C(C)(C)C)C3=NC=N1
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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.

试验操作

Cell experiment:[1]

Cell lines

Trypanosoma brucei(T. brucei) cells expressing only analogue-sensitive TbPLK (TbPLKas)

Reaction Conditions

0.5, 1 or 5 μM 3MB-PP1 for 12 h incubation

Applications

The growth of the TbPLKas cells was strongly inhibited at 1 and 5 μM, with a clear growth defect appearing 6 h after the addition of 3MB-PP1. At this point the cells ceased to divide for the duration of the experiment. This result showed that TbPLKascells treated with at least 1 μM 3MB-PP1 did not undergo cytokinesis within the first cell cycle. TbPLKascells treated with 500 nM drug grew at ~50% the rate of control cells.

Note

The technical data provided above is for reference only.

References:

1. Lozano-Núnez A, Ikeda KN, 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. Molecular Biology of the Cell, 2013, 24(9): 1321-1333.