PD98059 别名：PD 98059; PD‐98059
PD98059是一种非ATP竞争性的MEK抑制剂，IC50为2 μM，特异性抑制MEK-1介导的MAPK激活；PD98059 是一种 ERK1/2 信号的抑制剂。PD98059抑制ERK信号通路后，细胞内KAT2B蛋白的表达显着降低。
CAS No.：167869-21-8
Drug Dev Res. 2026 May;87:e70286.
Environ Pollut. 2025 Mar 03.
Long-term and low-dose exposure to triclosan induces POI phenotype in female offspring mice
Int Immunopharmacol. 2025 May 16;155:114615.
Cell Death Dis. 2024 Aug 01;15(8):555.
Neurourol Urodyn. 2024 Aug 16.
The SDF-1/CXCR4 axis is involved in adipose-derived stem cell migration
J Nanobiotechnology. 2022 Feb 2;20(1):65.
World J Gastroenterol. 2020 Jun 7;26(21):2810-2820.
Exp Cell Res. 2020 Jan 1;386(1):111719.
Environ Toxicol. 2020 Jun;35(6):673-682.
Exp Eye Res. 2018 Nov;176:10-19.
Rapamycin mediates mTOR signaling in reactive astrocytes and reduces retinal ganglion cell loss.
化学性质/溶解性/储存
| 分子量 | 267.28 |
| 分子式 | C16H13NO3 |
| CAS号 | 167869-21-8 |
| 溶解性（仅列举部分溶剂） | DMSO 20 mg/mL |
| 储存条件 | -20°C, dry, sealed, protect from light |
| 运输方式 | 冰袋运输，根据产品的不同，可能会有相应调整。 |
*不同实验中用到的溶剂可能不同，具体实验所需溶剂及溶解方法请参考相关文献描述。
生物活性
实验参考
下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.7414 mL | 18.707 mL | 37.4139 mL |
| 5 mM | 0.7483 mL | 3.7414 mL | 7.4828 mL |
| 10 mM | 0.3741 mL | 1.8707 mL | 3.7414 mL |
*吸湿的DMSO对产品的溶解度有显著影响，请使用新开封的DMSO；
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。
| 细胞系 | C-33 and C-81 cells |
| 方法 | Treatment with chemotherapeutic agents. Cells were seeded in 6-well culture plates in regular culture medium at a density of 2.5*105 and 1*105 cells/well for C-33 and C-81 cells, respectively, for 2 days and then fed with SR medium, i.e., PR-free RPMI-1640 medium containing 5% heat-inactivated CS-FBS, 1% glutamine and 0.5% gentamicin. Two days after steroid starvation, one set of attached cells was harvested and counted as day 0. The remaining cells were fed with fresh SR medium and treated with PD98059, U0126, vinorelbine, docetaxel or various combinations in which the dosage of each reagent was specified. Control cells were maintained in SR medium and received solvent alone without chemotherapeutic agents. Fresh SR medium with or without chemotherapeutic agents was added every 3 days. Treatment was continued for 3 or 6 days, as described in each figure legend. To quantify the inhibition of cell growth, attached cells were trypsinized and the cells counted with a Coulter counter. The number of cells in control sets that received solvent alone was designated as 100% for comparison. All experiments were done in triplicate and repeated at least twice. |
| 浓度 | 0~10 μM |
| 处理时间 | 3 or 6 days |
* 上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。
建议您制定动物给药及实验方案时，尽量参考已发表的相关实验文献（溶剂种类及配比众多，简单地溶解目的化合物，并不能解决动物给药依从性、体内生物利用度、组织分布等相关问题，未必能保证目的化合物在动物体内充分发挥生物学效用）。
体内实验的工作液，建议您现用现配，当天使用；如在配制过程中出现沉淀、析出现象，可以通过超声和（或）加热的方式助溶。
切勿一次性将产品全部溶解。
请在下面的计算器中，输入您的动物实验相关数据并点击计算，即可得到该实验的总需药量和工作液终浓度。
例如您给药剂量是10 mg/kg，平均每只动物的体重为20 g，每只动物的给药体积是100 μL，动物数量为20只，则该动物实验的总需药量为4 mg，工作液终浓度为2 mg/mL。
1：鉴于实验过程的损耗，建议您至少多配1-2只动物的量；
2：为该产品最终给药时的浓度。
| 动物模型 | acute lung injury in mice |
| 配制 | DMSO, then diluted with saline |
| 剂量 | 10mg/kg |
| 给药处理 | i. p. |
* 上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。
延伸阅读 （仅做信息扩展，不作实验参考）
PD98059（AbMole，M1822）是一种广泛应用于基础研究中的MEK1/2抑制剂，通过特异性抑制MEK1/2的激酶活性，从而阻断其下游ERK1/2的磷酸化，在多种细胞和动物模型中被用于解析ERK/MAPK信号通路的功能。
在体外实验中，PD98059（AbMole，M1822）常以10–25 μmol/L的浓度使用，例如在RAW 264.7巨噬细胞、EL-4淋巴细胞、HK-2近端肾小管上皮细胞、MDA-MB-231和MCF-7乳腺癌细胞、C666-1鼻咽癌细胞、U937单核细胞以及WJCMSCs和PDLSCs间充质干细胞中，该浓度范围可有效抑制ERK1/2磷酸化并调控细胞增殖、迁移、分化或凋亡等生物学过程[1-4]。在RAW 264.7细胞中，25 μmol/L PD98059不仅抑制ERK，还能促进破骨细胞分化[5]。此外，PD98059被发现能在小鼠神经干细胞中诱导星形胶质细胞生成，提示PD98059（CAS No.：167869-21-8）可用于调节神经干细胞的命运决定[6]。
在动物的体内研究中，PD98059（AbMole，M1822）可通过腹腔注射（如10 mg/kg）用于小鼠模型，显著提高血清IL-5水平，并在大鼠心肺复苏模型中以剂量依赖方式抑制脑皮层线粒体凋亡与自噬相关蛋白LC3-II和Beclin-1的表达[7, 8]。此外，在高血压诱导的主动脉重构小鼠模型中，PD98059被用于干预血管紧张素II（AngII，Angiotensin II）处理组，单独或与SO₂联用，结果发现PD98059可抑制ERK和磷酸化ERK（P-ERK）的表达，减轻主动脉壁增厚[9]。
综上，PD98059（AbMole，M1822）作为经典MEK1/2抑制工具，在小鼠、大鼠及多种人类和啮齿类细胞系中被广泛用于信号通路解析，其使用浓度和剂量需根据具体实验体系优化。
参考文献及鸣谢
J Nanobiotechnology. 2022 Feb 2;20(1):65.
AbMole的PD98059（AbMole，M1822）作为ERK1/2信号通路特异性抑制剂，在本研究中揭示了小鼠脊髓损伤后 ROS 诱导神经炎症的分子机制：即ROS/MAPK/NFκB P65 信号通路与上述炎症反应高度相关，提示该通路可作为脊髓损伤动物模型中的新型抑制靶点。
图来自J Nanobiotechnology. 2022 Feb 2;20(1):65.
参考文献及鸣谢
[1] Li, X.; Cao, X.; Zhang, X.; et al. MEK1/2 inhibitors induce interleukin-5 expression in mouse macrophages and lymphocytes. Biochemical and biophysical research communications 2016, 473 (4), 939-946.
[2] Nakamura, T.; Yoshida, E.; Hara, T.; et al. Zn(ii)2,9-dimethyl-1,10-phenanthroline stimulates cultured bovine aortic endothelial cell proliferation. RSC advances 2020, 10 (69), 42327-42337.
[3] Zhang, W.; Obuchi, S.; Teramura, Y. Analysis of cellular responses following interaction with extracellular vesicles derived from HEK293T and human adipose derived stem cells. Scientific reports 2025, 15 (1), 11835.
[4] Hasan, M.; Browne, E.; Guarinoni, L.; et al. Novel Melatonin, Estrogen, and Progesterone Hormone Therapy Demonstrates Anti-Cancer Actions in MCF-7 and MDA-MB-231 Breast Cancer Cells. Breast cancer : basic and clinical research 2020, 14, 1178223420924634.
[5] Agidigbi, T. S.; Kang, I. S.; Kim, C. Inhibition of MEK/ERK upregulates GSH production and increases RANKL-induced osteoclast differentiation in RAW 264.7 cells. Free radical research 2020, 54 (11-12), 894-905.
[6] Lee, H. R.; Lee, J.; Kim, H. J. Differential effects of MEK inhibitors on rat neural stem cell differentiation: Repressive roles of MEK2 in neurogenesis and induction of astrocytogenesis by PD98059. Pharmacological research 2019, 149, 104466.
[7] Hassan, R. M.; Elsayed, N. S.; Assaf, N.; et al. Limettin and PD98059 Mitigated Alzheimer's Disease Like Pathology Induced by Streptozotocin in Mouse Model: Role of p-ERK1/2/p-GSK-3beta/p-CREB/BDNF Pathway. Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology 2025, 20 (1), 55.
[8] Zheng, J. H.; Xie, L.; Li, N.; et al. PD98059 protects the brain against mitochondrial-mediated apoptosis and autophagy in a cardiac arrest rat model. Life sciences 2019, 232, 116618.
[9] Wu, H. J.; Huang, Y. Q.; Chen, Q. H.; et al. Sulfur Dioxide Inhibits Extracellular Signal-regulated Kinase Signaling to Attenuate Vascular Smooth Muscle Cell Proliferation in Angiotensin II-induced Hypertensive Mice. Chinese medical journal 2016, 129 (18), 2226-2232.
其他相关的MEK产品
参考文献
以上参考文献由AI整理，仅供参考，AbMole 尚未独立确认这些文献的准确性。
