PD 98059A selective inhibitor of MEK and blocker of MAPK

PD 98059 (CAS 167869-21-8)

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Solicitud: A selective inhibitor of MEK and blocker of MAPK
Número de CAS: 167869-21-8
Pureza: ≥98%
Peso Molecular: 267.28
Fórmula Molecular: C16H13NO3
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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.


References

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

Estado de Materia :
Solid
Solubilidad :
Soluble in DMSO (6.5 mg/ml), anhydrous DMSO (25 mg/ml), ethanol (0.6 mg/ml), dichloromethane, methanol, DMF (~20 mg/ml), and DMSO:PBS (1:9 pH7.2) (~0.25 mg/ml). Insoluble in 2-hydroxypropyl-β-cyclodextrin, water, and dilute aqueous acid.
ALMACENAMIENTO :
Store at -20° C
Punto de Fusión :
165-170° C
Punto de ebullición :
~453.1° C at 760 mmHg (Predicted)
Densidad :
~1.3 g/cm3 (Predicted)
Indice de Refracción :
n20D 1.65 (Predicted)
IC50 :
the increase in MAP kinase activity produced by NGF: IC50 = 2 µM; MEK1: IC50 = 4 µM; MEK2: IC50 = 50 µM; Serine/threonine-protein kinase RAF: IC50 = 2.8 µM (human); Cyclooxygenase-1: IC50 = 1 µM (human)
Valores de pK :
pKb: 1.21 (Predicted)
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
WGK Alemania :
3
PubChem CID :
4713
Número MDL :
MFCD00671789
SMILES :
COC1=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2

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PD 98059  Menciones del Producto

Ver como otros han utilizado PD 98059. Haga click en la entrada de PubMed .

Citaciones 1 a 10 de un total de 147

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: # 31076999  Jin, Y.|Wang, H.| et al. 2019. Neurotox Res.

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: # 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.

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: # 31071576  Li, Y.|Zuo, H.|Wang, H.|Hu, A.| et al. 2019. Biomed. Pharmacother. 116: 108749.

PMID: # 30783129  Klarström Engström, K. et al. 2019. Sci Rep. 9: 2296.

PMID: # 30976161  Shin, JH.|Kwon, HW.|Rhee, MH.|Park, HJ.| et al. 2019. J Ginseng Res. 43: 236-241.

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: # 30774310  Gao, S.|Lin, J.|Wang, T.|Shen, Y.|Li, Y.|Yang, W.|Zhou, K.|Hu, H.| et al. 2019. Drug Des Devel Ther. 13: 459-475.

Citaciones 1 a 10 de un total de 147
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