PD 98059 A selective inhibitor of MEK and blocker of MAPK

PD 98059 (CAS 167869-21-8)

PD 98059 | CAS 167869-21-8 is rated 5.0 out of 5 by 2.
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Synonym: 2′-Amino-3′-methoxyflavone
Application: A selective inhibitor of MEK and blocker of MAPK
CAS Number: 167869-21-8
Purity: ≥98%
Molecular Weight: 267.28
Molecular Formula: C16H13NO3
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
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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

Physical State :
Solid
Solubility :
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.
Storage :
Store at -20° C
Melting Point :
165-170° C
Boiling Point :
~453.1° C at 760 mmHg (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
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)
pK Values :
pKb: 1.21 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
Transport :
UN 2811, Class 6.1, Packing group III
PubChem CID :
4713
MDL Number :
MFCD00671789
SMILES :
COC1=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2

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PD 98059  Product Citations

See how others have used PD 98059. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 103 total

PMID: # 28753407  Hosokawa, Y. et al. 2017. Immunol. Invest. 46: 615-624.

PMID: # 27864646  Yan, X. et al. 2017. Lasers Med Sci. 32: 169-180.

PMID: # 28468003  Wang, Y. et al. 2017. Cell. Physiol. Biochem. 41: 2432-2446.

PMID: # 28627368  Gu, X. et al. 2017. Cell. Signal. 37: 103-114.

PMID: # 26718613  Liu, J. et al. 2016. Mol Med Rep. 13: 433-40.

PMID: # 27619995  Wu, Y. et al. 2016. J. Immunol.

PMID: # 26893689  Huang, Q. et al. 2016. Oncol Lett. 11: 1051-1056.

PMID: # 26913605  Chen, W. et al. 2016. Cell Death Dis. 7: e2115.

PMID: # 27302421  Li, Y. et al. 2016. Scientific reports. 6: 27911.

PMID: # 26875794  Xu, G. et al. 2016. J. Cell. Biochem. 117: 2118-27.

Citations 1 to 10 of 103 total
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Rated 5 out of 5 by from PD98059 the compound PD 98059 is worked very good for me and the product is cheaper compare to the ones available commercially
Date published: 2017-09-22
Rated 5 out of 5 by from PD98059 from SCBT (sc PD98059 from SCBT (sc-3532) was used to pre-treat HepG2, Hep3B and PLC/PRF/5 cells before exposure to galangin to study galangin's involvement in inducing endoplasmic reticulum stress (PubMed ID 24161691). -SCBT Publication Review
Date published: 2015-04-16
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