Name: PD98059
Brand: GlpBio
SKU: GC12819
Availability: InStock
Rating: 5 (22 reviews)

Product has been cited by 3 publications

Product Documents

Quality Control & SDS

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Purity: >98.00%

Protocol

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.

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.

Cas No.	167869-21-8	SDF
Synonyms	NSC 679828
Chemical Name	2-(2-amino-3-methoxyphenyl)chromen-4-one
Canonical SMILES	COC1=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2
Formula	C₁₆H₁₃NO₃	M.Wt	267.28
Solubility	≥ 40.23 mg/mL in DMSO	Storage	4°C, protect from light
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		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

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