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PD98059

Catalog No. T2623 CAS 167869-21-8

Synonyms: PD 98059

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.

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PD98059, CAS 167869-21-8

Pack Size	Availability	Price/USD
5 mg	In stock	$ 34.00
10 mg	In stock	$ 48.00
25 mg	In stock	$ 75.00
50 mg	In stock	$ 108.00
100 mg	In stock	$ 187.00
200 mg	In stock	$ 278.00
500 mg	In stock	$ 468.00
1 mL * 10 mM (in DMSO)	In stock	$ 53.00

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Purity: 100%

Purity: 99.66%

Purity: 98.56%

Purity: 98.52%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	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.
Targets&IC50	MEK2:50 μM (cell free), MEK1:2 μM (cell free)
In vitro	METHODS: Human breast cancer cells MCF-7 and MDA-MB-231 were treated with PD98059 (1-50 μM) for 12-72 h. Cell viability was detected using MTT. RESULTS: PD98059 dose-dependently and time-dependently inhibited the enhancement of breast cancer tumor cells. [1] METHODS: Multidrug-resistant tumor cells SMMC7721/ADM and BEL7402/ADM were treated with PD98059 (2.5-20 μM) for 1 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: PD98059 down-regulated pERK1/2 expression in cells in a dose-dependent manner. [2]
In vivo	METHODS: To test the effect on non-infectious shock, PD98059 (10 mg/kg) was administered intraperitoneally to CD mice with yeast polysaccharide-induced non-infectious shock. RESULTS: Treatment with PD98059 significantly reduced systemic toxicity, weight loss and mortality induced by yeast polysaccharide. [3] METHODS: To investigate the effects on experimental autoimmune encephalitis (EAE), PD98059 (5 mg/kg) was administered intraperitoneally once daily for two weeks to the SJL/J mouse model of EAE. RESULTS: PD98059 corrected immune dysfunction in EAE mice, which occurred concomitantly with the modulation of multiple signaling pathways. [4]
Kinase Assay	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].
Cell Research	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].
Animal Research	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].

Synonyms	PD 98059
Molecular Weight	267.28
Formula	C16H13NO3
CAS No.	167869-21-8

Storage

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

Solubility Information

Ethanol: 1.3 mg/mL (5 mM)

DMSO: 6.7 mg/mL (25 mM)

References and Literature

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.

Citations

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.

11. 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. Life Sciences. 2019 Mar 15;221:178-186 12. Li S, Deng G, Su J, et al. A novel all-trans retinoic acid derivative regulates cell cycle and differentiation of myelodysplastic syndrome cells by USO1. European Journal of Pharmacology. 2021: 174199. 13. Liu Z, Yang J. Uncarboxylated osteocalcin promotes osteogenic differentiation of mouse bone marrow–derived mesenchymal stem cells by activating the Erk‐Smad/β‐catenin signalling pathways. Cell Biochemistry and Function. 2019 14. Chen M S, Yang K S, Lin W C, et al. Lipofundin mediates major inhibition of intravenous propofol on phorbol myristate acetate and Escherichia coli-induced neutrophil extracellular traps. Molecular Biology Reports. 2022: 1-13 15. 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. European Journal of Pharmacology. 2019, 863: 172658 16. Zheng Y, Wang Y, Zhang X, et al. C19, a C-terminal peptide of CKLF1, decreases inflammation and proliferation of dermal capillaries in psoriasis. Scientific Reports. 2017, 7(1): 1-11 17. Yang Z, Guo D, Zhao J, et al.Aggf1 Specifies Hemangioblasts at the Top of Regulatory Hierarchy via Npas4l and mTOR-S6K-Emp2-ERK Signaling.Arteriosclerosis, Thrombosis, and Vascular Biology.2023

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Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Glutamine Metabolism Compound Library MAPK Inhibitor Library Ferroptosis Compound Library Anti-Pancreatic Cancer Compound Library NO PAINS Compound Library Anti-Liver Cancer Compound Library Apoptosis Compound Library

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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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