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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)
1mg电议
5mg电议
10mg电议

产品介绍
3MB-PP1 是一种大块嘌呤类似物，是一种 Polo 样激酶 1 (Plk1) 抑制剂。
Cas No.956025-83-5
别名4-氨基-1-叔丁基-3-(3-甲基苄基)吡唑并[3,4-D]嘧啶
化学名1-(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
分子式C17H21N5
分子量295.4
溶解度≤2mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.