PD98059（AbMole，M1822）是一種廣泛應(yīng)用于基礎(chǔ)研究中的MEK1/2抑制劑，通過特異性抑制MEK1/2的激酶活性，從而阻斷其下游ERK1/2的磷酸化，在多種細胞和動物模型中被用于解析ERK/MAPK信號通路的功能。

在體外實驗中，PD98059（AbMole，M1822）常以10–25 μmol/L的濃度使用，例如在RAW 264.7巨噬細胞、EL-4淋巴細胞、HK-2近端腎小管上皮細胞、MDA-MB-231和MCF-7乳腺癌細胞、C666-1鼻咽癌細胞、U937單核細胞以及WJCMSCs和PDLSCs間充質(zhì)干細胞中，該濃度范圍可有效抑制ERK1/2磷酸化并調(diào)控細胞增殖、遷移、分化或凋亡等生物學過程[1-4]。在RAW 264.7細胞中，25 μmol/L PD98059不僅抑制ERK，還能促進破骨細胞分化[5]。此外，PD98059被發(fā)現(xiàn)能在小鼠神經(jīng)干細胞中誘導星形膠質(zhì)細胞生成，提示PD98059（CAS No.：167869-21-8）可用于調(diào)節(jié)神經(jīng)干細胞的命運決定[6]。

在動物的體內(nèi)研究中，PD98059（AbMole，M1822）可通過腹腔注射（如10 mg/kg）用于小鼠模型，顯著提高血清IL-5水平，并在大鼠心肺復蘇模型中以劑量依賴方式抑制腦皮層線粒體凋亡與自噬相關(guān)蛋白LC3-II和Beclin-1的表達[7, 8]。此外，在高血壓誘導的主動脈重構(gòu)小鼠模型中，PD98059被用于干預血管緊張素II（AngII，Angiotensin II）處理組，單獨或與SO₂聯(lián)用，結(jié)果發(fā)現(xiàn)PD98059可抑制ERK和磷酸化ERK（P-ERK）的表達，減輕主動脈壁增厚[9]。

綜上，PD98059（AbMole，M1822）作為經(jīng)典MEK1/2抑制工具，在小鼠、大鼠及多種人類和嚙齒類細胞系中被廣泛用于信號通路解析，其使用濃度和劑量需根據(jù)具體實驗體系優(yōu)化。

參考文獻及鳴謝
J Nanobiotechnology. 2022 Feb 2;20(1):65.
AbMole的 PD98059（AbMole，M1822）作為ERK1/2信號通路特異性抑制劑，在本研究中揭示了小鼠脊髓損傷后 ROS 誘導神經(jīng)炎癥的分子機制：即ROS/MAPK/NFκB P65 信號通路與上述炎癥反應(yīng)高度相關(guān)，提示該通路可作為脊髓損傷動物模型中的新型抑制靶點。
參考文獻及鳴謝
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[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.