MEK1 Inhibitor (PD98059, 2

PD98059 (MEK1 Inhibitor) has been shown to act in vivo as a highly selective inhibitor of MEK1 activation and the MAP kinase cascade (1-4). PD98059 binds to the inactive forms of MEK1 and prevents activation by upstream activators such as c-Raf (3)\n\nSpecificity: \nInhibits activation of MEK1 and MEK2 with IC50 values of 4uM and 50uM, respectively (1-3). Testing has shown that PD98059 does not inhibit activation of other highly related dual-specificity protein kinases or the activity of over 18 other Ser/Thr protein kinases (3). As shown in the Western Blot, at concentrations up to 100uM PD98059 does not inhibit activation of MKK3 or SEK (MKK4) as determined by measuring phosphorylation at its activation site. We have also found no inhibition of MKK6 or related family members.\n\nApplications:\nSuitable for use in in vitro or cell-based assays. Other applications not tested.\n\nRecommended Dilution:\nMay be furhter diluted into aqueous buffers to yield desired concentrations \n(< 100uM) with final DMSO concentrations of ~0.1%. IC50 values for inhibitory activity against MEK1 are around 5пїЅ10uM. For experiments with cultured cells, pretreat with M2865-17A for one hour prior to stimulation.\nOptimal dilutions to be determined by the researcher.\n\nStorage and Stability:\nLyophilized powder may be stored at -20 degrees C. Stable for 12 months at -20 degrees C. Reconstitute with DMSO. Aliquot to avoid repeated freezing and thawing. Store at -20 degrees C. Reconstituted product is stable for 6 months at -20 degrees C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer

Prices direct from United States Biological

Quick response times

Exclusive Biosave savings/discounts

SPECIFICATIONS

Catalog Number

M2865-17A

Size

500ug

Applications

WB

Form

Supplied as a yellow, lyophilized powder. Reconstitution:\n20mM stock: 1.5mg/280ul DMSO or 50mM stock: 1.5mg/112ul DMSO.

References

1. Dudley, D.T., et al., Proc. Natl. Acad. Sci. USA 92: 7686-7689 (1995). 2. Pang, L., et al., J. Biol. Chem. 270: 13,585-13,588 (1995). 3. Alessi, D.R., et al., J. Biol. Chem. 270: 27,489-27,494 (1995). 4. Lazar, D.F., et al., J. Biol. Chem. 270: 20,801-20,807 (1995). 5. Runden, E., et al., J. Neurosci. 18: 7296-7305 (1998). 6. Veeranna, et al., J. Neurosci. 18: 4008-4021 (1998). 7. Xing, J., et al., Mol. Cell Biol. 18: 1946-1955 (1998).

Alternative Names

2-(2-amino-3-methoxyphenyl)-4H-1-Benzopyran-4-one; 2-(2'-Amino-3'-methoxy)-flavone; 2-(2-amino-3-methoxyphenyl)-chromone