PD98059

目录号: GC12819纯度: >98.00%同义词: 2-(2-氨基-3-甲氧基苯基)-4H-1-苯并吡喃-4-酮

D98059是一种有效的选择性MEK抑制剂，IC50为2 μM。

Cas No.: 167869-21-8

规格	价格	库存	数量
10mg	¥378.00	现货	1
50mg	¥756.00	现货	1
100mg	¥1,334.00	现货	1
10mM (in 1mL DMSO)	¥399.00	现货	1

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产品描述 Description

PD98059 is a potent and selective MEK inhibitor with an IC₅₀ of 2 μM. PD98059 binds to the inactive form of MEK, thereby preventing the upstream kinase from activating MEK1/2. Besides, PD98059 is a ligand for the AHR and functions as an AHR antagonist^[1-3].

PD98059(10 µM PD98059;14days) combined with TGF-β1 transforms human UDSCs (hUDSCs) into smooth muscle cells (SMCs)^[4]. PD98059 (10 μM PD98059 ;24 h) suppresses the ERK pathway and the epithelial mesenchymal transition process(EMT) process in low dose cisplatin-resistant ovarian cancer cells(SKOV-3/DDP)^[5]. PD98059 arrested Hec50co cells at the G0/G1 phase, the combination with PTX treatment increased accumulation at both the G0/G1 and G2/M phase^[6]. PD98059(1, 5, 10, 20 and 50 µM；24h) inhibited MCF-7 and MDA-MB-231 cells proliferation in a dose-dependent manner^[7].

PD98059(5 mg/kg/day; i.p; 2 weeks) treatment reduced adverse effects, including micronucleus (MN) formation, lipid peroxidation, and glutathione(GSH) oxidation in the EAE model^[8].PD98059(0.15/0.3mg/kg PD98059; i.v. gtt) protects the brain against mitochondrial-mediated apoptosis and autophagy at 24 h post-resuscitation in rats subjected to cardiac arrest/cardiopulmonary resuscitation (CA/CPR), which is linked with the downregulation of dynamin-related protein 1 (Drp1) expression^[9]. Treatment of mice with PD98059(10mg/kg; i.p; bolus) attenuated the peritoneal exudation and the migration of polymorphonuclear cells caused by zymosan^[10].

References:

[1]. Reiners JJ Jr, Lee JY, Clift RE, et.al. PD98059 is an equipotent antagonist of the aryl hydrocarbon receptor and inhibitor of mitogen-activated protein kinase kinase. Mol Pharmacol. 1998 Mar;53(3):438-45. doi: 10.1124/mol.53.3.438. PMID: 9495809.

[2]. Dudley DT, Pang L, et.al. A synthetic inhibitor of the mitogen-activated protein kinase cascade. Proc Natl Acad Sci U S A. 1995 Aug 15;92(17):7686-9. doi: 10.1073/pnas.92.17.7686. PMID: 7644477; PMCID: PMC41210.

[3]. Attia SM, Ahmad SF, et.al.The MAP kinase inhibitor PD98059 reduces chromosomal instability in the autoimmune encephalomyelitis SJL/J-mouse model of multiple sclerosis. Mutat Res Genet Toxicol Environ Mutagen. 2021 Jan-Feb;861-862:503278. doi: 10.1016/j.mrgentox.2020.503278. Epub 2020 Oct 29. PMID: 33551096.

[4]. Hwang Y, Cha SH, et.al.Combination of PD98059 and TGF-β1 Efficiently Differentiates Human Urine-Derived Stem Cells into Smooth Muscle Cells. Int J Mol Sci. 2021 Sep 29;22(19):10532. doi: 10.3390/ijms221910532. PMID: 34638875; PMCID: PMC8508912.

[5]. Hou L, Hou X, et.al.PD98059 impairs the cisplatin-resistance of ovarian cancer cells by suppressing ERK pathway and epithelial mesenchymal transition process. Cancer Biomark. 2017 Dec 12;21(1):187-194. doi: 10.3233/CBM-170644. PMID: 29103028.

[6].Wiwatchaitawee K, Mekkawy AI, et.al. The MEK 1/2 inhibitor PD98059 exhibits synergistic anti-endometrial cancer activity with paclitaxel in vitro and enhanced tissue distribution in vivo when formulated into PAMAM-coated PLGA-PEG nanoparticles. Drug Deliv Transl Res. 2022 Jul;12(7):1684-1696. doi: 10.1007/s13346-021-01065-7. Epub 2021 Oct 11. PMID: 34635984; PMCID: PMC8995400.

[7]. Zhao Y, Ge CC, et.al. MEK inhibitor, PD98059, promotes breast cancer cell migration by inducing β-catenin nuclear accumulation. Oncol Rep. 2017 Nov;38(5):3055-3063. doi: 10.3892/or.2017.5955. Epub 2017 Sep 13. PMID: 29048617.

[8]. Attia SM, Ahmad SF, et.al.The MAP kinase inhibitor PD98059 reduces chromosomal instability in the autoimmune encephalomyelitis SJL/J-mouse model of multiple sclerosis. Mutat Res Genet Toxicol Environ Mutagen. 2021 Jan-Feb;861-862:503278. doi: 10.1016/j.mrgentox.2020.503278. Epub 2020 Oct 29. PMID: 33551096.

[9]. Zheng JH, Xie L, et.al. PD98059 protects the brain against mitochondrial-mediated apoptosis and autophagy in a cardiac arrest rat model. Life Sci. 2019 Sep 1;232:116618. doi: 10.1016/j.lfs.2019.116618. Epub 2019 Jun 29. PMID: 31265854.

[10].Di Paola R, Galuppo M, 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. doi: 10.1016/j.phrs.2009.09.008. Epub 2009 Oct 9. PMID: 19819333.

D98059是一种有效的选择性MEK抑制剂,IC₅₀为2 μM。PD98059结合无活性形式的MEK,从而阻止上游激酶激活MEK1/2。此外,PD98059是AHR的配体,具有AHR拮抗剂的功能^[1-3]。

PD98059(10 µM PD98059;14days)结合TGF-β1可将人尿源干细胞HUDSCs转化为平滑肌细胞(SMCs)^[4]。PD98059 (10 μM PD98059 ;24 h)抑制低剂量顺铂耐药卵巢癌细胞(SKOV-3/DDP)的ERK通路和上皮间充质转化EMT过程^[5]。PD98059在G0/G1期阻滞了Hec50co细胞,与PTX联合处理增加了G0/G1和G2/M期的积累^[6]。PD98059(1、5、10、20 and 50µM;24h)呈剂量依赖性抑制MCF-7和MDA-MB-231细胞的增殖^[7]。

在EAE模型中,PD98059(5 mg/kg/day; i.p; 2 weeks)治疗减少了不良反应,包括微核(MN)形成、脂质过氧化和谷胱甘肽(GSH)氧化^[8]。在心脏骤停/心肺复苏(CA/CPR)大鼠复苏后24小时,PD98059(0.15/0.3mg/kg PD98059; i.v. gtt)保护大脑免受线粒体介导的细胞凋亡和自噬,这与动力蛋白相关蛋白1 (Drp1)表达下调有关^[9]。用PD98059(10mg/kg; i.p; bolus)治疗小鼠可减少由zymosan酶引起的腹膜渗出和多形核细胞的迁移^[10]。

实验参考方法 Experimental Reference Method

Kinase activity Assay^[1]：
Preparation method	Incorporation of ³²P into myelin basic protein (MBP) was assayed in the presence of glutathione S-transferase (GST) fusion proteins containing the 44-kDa MAPK (GST-MAPK) or the 45-kDa MEK (GST-MEK1) with(or not) PD98059. Assays were conducted in 50 μl of 50 mM Tris, pH 7.4，10 mM MgCl₂，2 mM EGTA，10 μM ^[y-32P]ATP containing 10 μg of GST-MEK1, 0.5 μg of GST-MAPK, and 40 μg of MBP. After incubation at 30℃ for 15 min, reactions were stopped by addition of Laemmli SDS sample buffer. Phosphorylated MBP was resolved by SDS/PAGE(10%).
Applications	D98059 is a non-ATP-competitive MEK inhibitor with an IC₅₀ of 2 μM.
Cell experiment ^[2]:
Cell lines	MCF-7 and MDA-MB-231 cells
Preparation method	Cells were seeded in 96-well plates. After cells grew to 30% of the bottom of cell culture plates, various concentrations of PD980589 (1, 5, 10, 20 and 50 µM) were added to the cells and incubation was carried out for 24 h.
Reaction Conditions	1, 5, 10, 20 and 50 µM；24h
Applications	PD98059 inhibited MCF-7 and MDA-MB-231 cells proliferation in a dose-dependent manner.
Animal experiment ^[3]:
Animal models	SJL/J mice (experimental autoimmune encephalomyelitis (EAE) model)
Preparation method	Mice received a single daily intraperitoneal injection of PD98059, or sham with equal amounts of 1% DMSO, once they reached a neurological disability score of >2 (i.e., day 14). Mice were euthanized 24 h after the last injection with PD98059, and bone marrow cells and spinal cord tissues were harvested.
Dosage form	5 mg/kg/day; i.p; 2 weeks
Applications	PD98059 treatment reduced adverse effects, including micronucleus (MN) formation, lipid peroxidation, and glutathione (GSH) oxidation in the EAE model.
References: [1]. Dudley DT, Pang L, et.al. A synthetic inhibitor of the mitogen-activated protein kinase cascade. Proc Natl Acad Sci U S A. 1995 Aug 15;92(17):7686-9. doi: 10.1073/pnas.92.17.7686. PMID: 7644477; PMCID: PMC41210. [2]. Zhao Y, Ge CC, et.al.MEK inhibitor, PD98059, promotes breast cancer cell migration by inducing β-catenin nuclear accumulation. Oncol Rep. 2017 Nov;38(5):3055-3063. doi: 10.3892/or.2017.5955. Epub 2017 Sep 13. PMID: 29048617. [3]. Attia SM, Ahmad SF, et.al. The MAP kinase inhibitor PD98059 reduces chromosomal instability in the autoimmune encephalomyelitis SJL/J-mouse model of multiple sclerosis. Mutat Res Genet Toxicol Environ Mutagen. 2021 Jan-Feb;861-862:503278. doi: 10.1016/j.mrgentox.2020.503278. Epub 2020 Oct 29. PMID: 33551096.

产品文档 Product Documents

批次：Purity:>98.00%

化学性质Chemical Properties

CAS 号

167869-21-8

同义词

2-(2-氨基-3-甲氧基苯基)-4H-1-苯并吡喃-4-酮

化学名

2-(2-amino-3-methoxyphenyl)chromen-4-one

SMILES

COC1=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2

分子式

C₁₆H₁₃NO₃

分子量

267.28 g/mol

溶解性

≥ 40.23 mg/mL in DMSO

保存条件

4°C, protect from light

General tips

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储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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