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PD98059

PD98059

产品编号 T2623   CAS 167869-21-8
别名: PD 98059

PD98059 是一种 MEK 抑制剂,抑制 MEK1 和 MEK2 (IC50=2/50 μM),具有非 ATP 竞争性。PD98059 也是一种 AHR 的配体而起拮抗作用。PD98059 可以抑制细胞自噬

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PD98059 Chemical Structure
PD98059, CAS 167869-21-8
规格 价格/CNY 货期 数量
1 mg ¥ 279 现货
2 mg ¥ 397 现货
5 mg ¥ 598 现货
10 mg ¥ 893 现货
25 mg ¥ 1,650 现货
50 mg ¥ 2,610 现货
100 mg ¥ 3,470 现货
200 mg ¥ 4,570 现货
500 mg ¥ 6,820 现货
1 g ¥ 8,660 现货
1 mL * 10 mM (in DMSO) ¥ 697 现货
产品目录号及名称: PD98059 (T2623)
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纯度: 100%
纯度: 99.66%
纯度: 98.56%
纯度: 98.52%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2/50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.
靶点活性 MEK2:50 μM (cell free), MEK1:2 μM (cell free)
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]
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]
激酶实验 c-Raf and MEK kinase were measured by their ability to activate MAPKK1 (or MAPKK2) in a 30-min coupled assay containing MAPKK1 (or MAPKK2) and its substrate p42 MAP kinase. One unit of c-Raf or MEK kinase activity was that amount which increased the activity of p42Graphic by 1 unit/min. MAPKK was assayed directly in the cell lysate by the activation of bacterially expressed p42Graphic. One unit of MAPKK was that amount which increased the activity of p42Graphic by 1 unit/min. The assays of c-Raf and MAPKK are quantitative and extremely sensitive and are detailed elsewhere. p42Graphic was assayed by its ability to phosphorylate myelin basic protein and MAPKAP kinase 1 α/β by the phosphorylation of a peptide related to the C terminus of ribosomal protein S6 [Gly-245, Gly-246]S6-(218-249). One unit of p42Graphic or MAPKAP kinase-1α/β was that amount which catalyzed the phosphorylation of 1 nmol of substrate peptide in 1 min. Protein kinase activities in immunoprecipitates were measured by adding the other assay components to the tubes containing the immunoprecipitated enzyme [1].
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].
别名 PD 98059
分子量 267.28
分子式 C16H13NO3
CAS No. 167869-21-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 1.3 mg/mL (5 mM)

DMSO: 6.7 mg/mL (25 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 3.7414 mL 18.707 mL 37.4139 mL 93.5349 mL
5 mM 0.7483 mL 3.7414 mL 7.4828 mL 18.707 mL
DMSO 10 mM 0.3741 mL 1.8707 mL 3.7414 mL 9.3535 mL
20 mM 0.1871 mL 0.9353 mL 1.8707 mL 4.6767 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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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. 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. 3. 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. 4. 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. 5. 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. 6. 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. 7. 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. 8. 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. 9. 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. 10. Dong L, Gong J, Wang Y, et al. Chiral geometry regulates stem cell fate and activity[J]. Biomaterials. 2019: 119456.

文献引用

1. Xu X, Song L, Li Y, et al.Neurotrophin-3 promotes peripheral nerve regeneration by maintaining a repair state of Schwann cells after chronic denervation via the TrkC/ERK/c-Jun pathway.Journal of Translational Medicine.2023, 21(1): 1-20. 2. Zou X, Zeng M, Zheng Y, et al.Comparative Study of Hydroxytyrosol Acetate and Hydroxytyrosol in Activating Phase II Enzymes.Antioxidants.2023, 12(10): 1834. 3. Urade R, Chang W T, Ko C C, et al.A fluorene derivative inhibits human hepatocellular carcinoma cells by ROS-mediated apoptosis, anoikis and autophagy.Life Sciences.2023: 121835. 4. Liu Y, Yuan C, Zhou M, et al. Co-cultured Bone-marrow Derived and Tendon Stem Cells: Novel Seed Cells for Bone Regeneration. Open Life Sciences. 2019, 14(1): 568-575 5. 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. International Journal of Molecular Sciences. 2020, 21(15): 5362 6. Li P, Lin Q, Sun S, et al. Inhibition of cannabinoid receptor type 1 sensitizes triple-negative breast cancer cells to ferroptosis via regulating fatty acid metabolism. Cell Death & Disease. 2022, 13(9): 1-15. 7. Dong L, Gong J, Wang Y, et al. Chiral geometry regulates stem cell fate and activity. Biomaterials. 2019: 119456. 8. Su J W, Li S F, Tao J J, et al. Estrogen protects against acidosis-mediated articular chondrocyte injury by promoting ASIC1a protein degradation. European Journal of Pharmacology. 2021: 174381. 9. Hu Q, Du H, Ma G, et al. Purification, identification and functional characterization of an immunomodulatory protein from Pleurotus eryngii. Food & Function. 2018, 9(7): 3764-3775 10. Chen M S, Tung Y W, Hu C L, et al. Three Lipid Emulsions Reduce Staphylococcus aureus-Stimulated Phagocytosis in Mouse RAW264. 7 Cells. Microorganisms. 2021, 9(12): 2479.
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相关化合物库

该产品包含在如下化合物库中:
酪氨酸激酶分子库 免疫/炎症分子化合物库 抗癌化合物库 细胞凋亡化合物库 MAPK 抑制剂库 HIF-1化合物库 已知活性化合物库 抑制剂库 抗肥胖化合物库 抗衰老化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

PD98059 167869-21-8 Autophagy Immunology/Inflammation MAPK ERK Aryl Hydrocarbon Receptor MEK AhR Extracellular signal regulated kinases MAP2K MAPKK inhibit Mitogen-activated protein kinase kinase Inhibitor PD-98059 PD 98059 inhibitor

 

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