PD98059

CAS号

167869-21-8

分子式

C16H13NO3

主要靶点

ERK|MEK|Aryl Hydrocarbon Receptor|Autophagy

仅限科研使用

Cat No : CM05068

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Synonyms

ERK|Extracellular signal regulated kinases|AhR|ArylHydrocarbonReceptor|Aryl Hydrocarbon Receptor|Autophagy|inhibit|Inhibitor|MEK1|MEK|Mitogen-activated protein kinase kinase|MAP2K|MAPKK|PD98059|PD-98059|PD 98059



产品信息

CAS号 167869-21-8
分子式 C16H13NO3
主要靶点 ERK|MEK|Aryl Hydrocarbon Receptor|Autophagy
主要通路 MAPK 信号通路|免疫与炎症|MAPK 信号通路|自噬
分子量 267.28
纯度 100%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 ERK|Extracellular signal regulated kinases|AhR|ArylHydrocarbonReceptor|Aryl Hydrocarbon Receptor|Autophagy|inhibit|Inhibitor|MEK1|MEK|Mitogen-activated protein kinase kinase|MAP2K|MAPKK|PD98059|PD-98059|PD 98059

靶点活性

MEK2:50 μM (cell free)|MEK1:2 μM (cell free)

体内活性

方法:为检测对非感染性休克的影响,将 PD98059 (10 mg/kg) 腹腔注射给酵母多糖诱导非感染性休克的 CD 小鼠。 结果:用 PD98059 治疗显著降低了酵母多糖引起的全身毒性、体重减轻和死亡率。[3] 方法:为研究对实验性自身免疫性脑炎 (EAE) 的作用,将 PD98059 (5 mg/kg) 腹腔注射给 EAE 的 SJL/J 小鼠模型,每天一次,持续两周。 结果:PD98059 可以纠正 EAE 小鼠的免疫功能障碍,这与多种信号通路的调节同时发生。[4]

体外活性

方法:人乳腺癌细胞 MCF-7 和 MDA-MB-231 用 PD98059 (1-50 μM) 处理 12-72 h,使用 MTT 方法检测细胞活力。 结果:PD98059 剂量依赖性和时间依赖性抑制乳腺癌肿瘤细胞增强。[1] 方法:多药耐药性肿瘤细胞 SMMC7721/ADM 和 BEL7402/ADM 用 PD98059 (2.5-20 μM) 处理 1 h,使用 Western Blot 方法检测靶点蛋白表达水平。 结果:PD98059 用剂量依赖性方式下调细胞中的 pERK1/2 表达率。[2]

溶解度

10% DMSO+40% PEG300+5% Tween 80+45% Saline:0.67 mg/mL (2.51 mM);DMSO:13.75 mg/mL (51.44 mM);Ethanol:1.3 mg/mL (5 mM)

细胞实验

The MCF10A-Neo and MCF10A-NeoT lines were derived by transfection of the MCF10A cell line with the pHo6 plasmid and the pHo6 plasmid containing an Ha-ras oncogene derived from the human T24 bladder carcinoma cell line, and subsequent selection for resistance to G418. The transfected lines represent pooled survivors, as opposed to clonal lines. With the exception of the EGF content being increased from 10 to 20 ng/ml, the cells were cultured in supplemented Dulbecco's modified Eagle's medium/Ham's F-12 medium in a humidified atmosphere of 95% air/5% CO2 at 37°C. Subconfluent cultures were treated with varying concentrations of chemicals dissolved in DMSO (absolute volume of solvent < 0.1% of medium volume). Subconfluent cultures are treated with PD98059 (0-100 μM). Viability of cells after treatment was assessed by ability to exclude trypan blue. Cultures earmarked for RNA isolation were washed twice with phosphate-buffered saline (2.7 mM KCl, 1.5 mM KH2PO4, 137mM NaCl, 8 mM Na2HPO4, pH 7.2) at harvesting and stored at 280°C [2].

动物实验

Mice were randomized into 4 groups (n= 40 animals/group): (i) CAR + vehicle group. Mice were subjected to carrageenan-induced pleurisy and received the vehicle for PD98059 (10% dimethylsulfoxide (DMSO) (v/v) i.p. bolus 1 h after carrageen administration(N=10); (ii) PD98059 group. Same as the CAR + vehicle group but were administered PD98059 (10 mg/kg, i.p. bolus) 1 h after carrageenan administration (N=10); (iii) Sham+saline group. Sham-treated group in which identical surgical procedures to the CAR group were performed, except that the saline was administered instead of carrageenan (n=10); (iv) Sham+ PD98059 group. Identical to Sham+saline group except for the administration of PD98059 (10 mg/kg i.p. bolus) 1h after carrageenan administration of saline (N=10). The doses of PD98059 (10 mg/kg) used here were based on previous in vivo studies that demonstrated regulation of the inflammation process [4].

参考文献

1.Zhao Y, et al. MEK inhibitor, PD98059, promotes breast cancer cell migration by inducing β-catenin nuclear accumulation. Oncol Rep. 2017 Nov;38(5):3055-3063.
2.Dong L, Gong J, Wang Y, et al. Chiral geometry regulates stem cell fate and activity[J]. Biomaterials. 2019: 119456.
3.Chen S, et al. Reversing multidrug resistance in hepatocellular carcinoma cells by inhibiting extracellular signal-regulated kinase/mitogen-activated protein kinase signaling pathway activity. Oncol Lett. 2014 Nov;8(5):2333-2339.
4.Di Paola R, et al. PD98059, a specific MAP kinase inhibitor, attenuates multiple organ dysfunction syndrome/failure (MODS) induced by zymosan in mice. Pharmacol Res. 2010 Feb;61(2):175-87.
5.Ahmad SF, et al. MAP kinase inhibitor PD98059 regulates Th1, Th9, Th17, and natural T regulatory cells in an experimental autoimmune encephalomyelitis mouse model of multiple sclerosis. Eur J Pharmacol. 2023 Nov 15;959:176086.
6.Yeh H T, Tsai Y S, Chen M S, et al. Flavopereirine induces cell cycle arrest and apoptosis via the AKT/p38 MAPK/ERK1/2 signaling pathway in human breast cancer cells[J]. European Journal of Pharmacology. 2019: 172658.
7.Chen M S, Lin W C, Yeh H T, et al. Propofol specifically reduces PMA-induced neutrophil extracellular trap formation through inhibition of p-ERK and HOCl[J]. Life sciences. 2019 Mar 15;221:178-186.
8.Hu, Qiuhui, Hengjun Du, Gaoxing Ma, Fei Pei, Ning Ma, Biao Yuan, Paul A. Nakata, and Wenjian Yang. Purification, identification and functional characterization of an immunomodulatory protein from Pleurotus eryngii [J]. Food Funct. 2018 Jul 17;9(7):3764-3775.
9.Chen M S, Yeh H T, Li Y Z, et al. Flavopereirine Inhibits Autophagy via the AKT/p38 MAPK Signaling Pathway in MDA-MB-231 Cells[J]. International Journal of Molecular Sciences. 2020, 21(15): 5362.
10.Zheng Y, Wang Y, Zhang X, et al. C19, a C-terminal peptide of CKLF1, decreases inflammation and proliferation of dermal capillaries in psoriasis[J]. Scientific Reports. 2017 Oct 24;7(1):13890.

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