PD98059
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PD98059是一种选择性的和可逆的MAPK激活酶（MAPK/ERK激酶、MEK）抑制剂，作用于基底MEK（GST-MEK1）和部分激活的MEK（218和222残基由丝氨酸突变为谷氨酸，GST-MEK-2E），IC50值为10 μM [1]。
与DMSO处理的对照细胞相比，PD98059导致细胞形态和密度的明显变化。在人白血病U937细胞中，PD98059抑制细胞增殖，诱导细胞死亡。此外，PD98059剂量依赖地抑制ERK1/2的磷酸化，下调cyclin E/Cdk2和cyclin D1/Cdk4的水平，导致G1期停滞和凋亡诱导[2]。
参考文献：
[1] Dudley DT1,?Pang L,?Decker SJ,?Bridges AJ,?Saltiel AR. A synthetic inhibitor of the mitogen-activated protein kinase cascade. Proc Natl Acad Sci U S A.?1995 Aug 15;92(17):7686-9.
[2] Moon DO1,?Park C,?Heo MS,?Park YM,?Choi YH,?Kim GY. PD98059 triggers G1 arrest and apoptosis in human leukemic U937 cells through downregulation of Akt signal pathway. Int Immunopharmacol.?2007 Jan;7(1):36-45. Epub 2006 Sep 8.
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| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 267.28 |
| Cas No. | 167869-21-8 |
| Formula | C16H13NO3 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥40.23 mg/mL in DMSO |
| Chemical Name | 2-(2-amino-3-methoxyphenyl)chromen-4-one |
| SDF | Download SDF |
| Canonical SMILES | COC1=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。 |
| 细胞实验 [1]: | |
|
细胞系 |
C-81LNCaP细胞（传代80-120代的LNCaP细胞） |
|
溶解方法 |
该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液，一般步骤如下：请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
|
反应条件 |
10 μM, 3天 |
|
实验结果 |
用10 μM的PD98059作为单一试剂处理C-81LNCaP细胞，使Bax蛋白的含量升高5倍，而单独使用1.2 nMdocetaxel仅使之升高2倍。10 μM PD98056与1.2 nMdocetaxel组合使用引起Bcl-2的磷酸化失活，使Bax表达升高15倍，此外，两种化合物的组合使用消除Bcl-XL的升高。这些组合效应与凋亡细胞的大量增加相关，可能对细胞生长产生大约20％的额外抑制作用。 |
| 动物实验 [2]: | |
|
动物模型 |
雄性 SV-129 小鼠 |
|
剂量 |
脑室内注射，200 μM |
|
实验结果 |
使用PD98059处理小鼠30分钟诱导缺血。使用PD98059预处理减少缺血2小时和再灌注3分钟后MCA区域皮质中磷酸ERK1/2的免疫染色。PD98059还可以将梗死面积减小55％。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Zelivianski S, Spellman M, Kellerman M, et al. ERK inhibitor PD98059 enhances docetaxel-induced apoptosis of androgen-independent human prostate cancer cells. International journal of cancer, 2003, 107(3): 478-485. [2] Alessandrini A, Namura S, Moskowitz M A, et al. MEK1 protein kinase inhibition protects against damage resulting from focal cerebral ischemia. Proceedings of the National Academy of Sciences, 1999, 96(22): 12866-12869. |
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| 描述 | PD98059是一种选择性的和可逆的MAPK激活酶（MEK）抑制剂，作用于基底MEK（GST-MEK1）和部分激活的MEK（218和222残基由丝氨酸突变为谷氨酸，GST-MEK-2E），IC50值均为约10 μM。 | |||||
| 靶点 | GST-MEK1 | GST-MEK-2E) | ||||
| IC50 | 10 μM | 10 μM | ||||
质量控制和MSDS
- 批次：
化学结构
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