3MB-PP1
(Synonyms: 4-氨基-1-叔丁基-3-(3-甲基苄基)吡唑并[3,4-D]嘧啶) 目录号 : GC14186An inhibitor of analog-sensitive Plk1 alleles
Cas No.:956025-83-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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 | |
| 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 SMILES | NC1=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°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。