PD 98059 is a potent, selective and reversible cell permeable inhibitor of MEK-1 (MAPKK1 or MAPKs ) that binds to the inactive form of MEK-1, blocking MEK-1 activation and leading to inhibition of phosphorylation and the activation of MAP kinase. In PC12 pheochromocytoma cells, it produced complete blockage of any increase in MAPK activity (IC50 = 2 μM) produced by nerve growth factor. It has been shown to enhance self-renewal of embryonic stem cells and has been used to unravel the role of the MAPK cascade in biological systems. The compound has been reported to induce GSTA2 (glutathione S-transferase A2) production in H4IIE cells. PD 98059 has also been shown to enhance insulin-mediated increase in glutathione levels as well as, independent of MEK1 inhibition, elevate primary cultured rat hepatocyte glutathione levels.
1. Alessi, D R., et al., 1995. PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo. The Journal of biological chemistry. 270(46): 27489-94. PMID: 7499206
2. Dudley, D T., et al., 1995. A synthetic inhibitor of the mitogen-activated protein kinase cascade. Proceedings of the National Academy of Sciences of the United States of America. 92(17): 7686-9. PMID: 7644477
3. Cuenda, A., et al., 1995. SB 203580 is a specific inhibitor of a MAP kinase homologue which is stimulated by cellular stresses and interleukin-1. FEBS letters. 364(2): 229-33. PMID: 7750577
4. Pang, L., et al., 1995. Inhibition of MAP kinase kinase blocks the differentiation of PC-12 cells induced by nerve growth factor. The Journal of biological chemistry. 270(23): 13585-8. PMID: 7775407
5. Tsang, F., et al., 1998. Effects of mitogen-activated protein kinase kinase inhibitor PD 098059 on antigen challenge of guinea-pig airways in vitro. British journal of pharmacology. 125(1): 61-8. PMID: 9776345
6. Badache, A., et al., 2001. Interleukin 6 inhibits proliferation and, in cooperation with an epidermal growth factor receptor autocrine loop, increases migration of T47D breast cancer cells. Cancer research. 61(1): 383-91. PMID: 11196191
7. Kang, Keon Wook., et al., 2003. Activation of CCAAT/enhancer-binding protein beta by 2′-amino-3′-methoxyflavone (PD98059) leads to the induction of glutathione S-transferase A2. Carcinogenesis. 24(3): 475-82. PMID: 12663507
8. Qi, Xiaoxia., et al., 2004. BMP4 supports self-renewal of embryonic stem cells by inhibiting mitogen-activated protein kinase pathways. Proceedings of the National Academy of Sciences of the United States of America. 101(16): 6027-32. PMID: 15075392
9. Kim, Sang K., et al., 2004. Insulin signaling regulates gamma-glutamylcysteine ligase catalytic subunit expression in primary cultured rat hepatocytes. The Journal of pharmacology and experimental therapeutics. 311(1): 99-108. PMID: 15169830
10. Kim, Sang K., et al., 2006. The mitogen-activated protein kinase kinase (mek) inhibitor PD98059 elevates primary cultured rat hepatocyte glutathione levels independent of inhibiting mek. Drug metabolism and disposition: the biological fate of chemicals. 34(4): 683-9. PMID: 16443668
11. Kojima, Kensuke., et al., 2007. Mitogen-activated protein kinase kinase inhibition enhances nuclear proapoptotic function of p53 in acute myelogenous leukemia cells. Cancer research. 67(7): 3210-9. PMID: 17409429
See how others have used PD 98059 (CAS 167869-21-8). Click on the entry to view the PubMed entry .
PMID: # 30886861 Tsai, FM.|Li, CH.|Wang, LK.|Chen, ML.|Lee, MC.|Lin, YY.|Wang, CH.| et al. 2019. Biomed Res Int. 2019: 6360503.
PMID: # 31071576 Li, Y.|Zuo, H.|Wang, H.|Hu, A.| et al. 2019. Biomed. Pharmacother. 116: 108749.
PMID: # 31278313 De Nuccio, C.|Bernardo, A.|Ferrante, A.|Pepponi, R.|Martire, A.|Falchi, M.|Visentin, S.|Popoli, P.|Minghetti, L.| et al. 2019. Sci Rep. 9: 9782.
PMID: # 31423275 Jiang, L.|Meng, W.|Yu, G.|Yin, C.|Wang, Z.|Liao, L.|Meng, F.| et al. 2019. Oncol Lett. 18: 2034-2042.
PMID: # 30679767 Han, R.|Hu, S.|Qin, W.|Shi, J.|Zeng, C.|Bao, H.|Liu, Z.| et al. 2019. Sci Rep. 9: 716.
PMID: # 31155290 Shu, S.|Zhang, Y.|Li, W.|Wang, L.|Wu, Y.|Yuan, Z.|Zhou, J.| et al. 2019. Biochem. Biophys. Res. Commun. 515: 378-385.
PMID: # 30976161 Shin, JH.|Kwon, HW.|Rhee, MH.|Park, HJ.| et al. 2019. J Ginseng Res. 43: 236-241.
PMID: # 30783129 Klarström Engström, K. et al. 2019. Sci Rep. 9: 2296.
PMID: # 30370560 Fujihara, C.|Kanai, Y.|Masumoto, R.|Kitagaki, J.|Matsumoto, M.|Yamada, S.|Kajikawa, T.|Murakami, S.| et al. 2019. J. Cell. Physiol. 234: 7149-7160.
PMID: # 31272829 Fang, MY.|Markmiller, S.|Vu, AQ.|Javaherian, A.|Dowdle, WE.|Jolivet, P.|Bushway, PJ.|Castello, NA.|Baral, A.|Chan, MY.|Linsley, JW.|Linsley, D.|Mercola, M.|Finkbeiner, S.|Lecuyer, E.|Lewcock, JW.|Yeo, GW.| et al. 2019. Neuron.
Santa Cruz Biotechnology, Inc. is a world leader in the development of products for the biomedical research market. Call us Toll Free at 1-800-457-3801.
Copyright © 2007-2020 Santa Cruz Biotechnology, Inc. All Rights Reserved. "Santa Cruz Biotechnology", and the Santa Cruz Biotechnology, Inc. logo, "Santa Cruz Animal Health", "San Juan Ranch", "Supplement of Champions", the San Juan Ranch logo, "Ultracruz", "Chemcruz", "Immunocruz", "Exactacruz", and "EZ Touch" are registered trademarks of Santa Cruz Biotechnology, Inc.
All trademarks are the property of their respective owners.