MEK1 Inhibitor (PD98059),

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), Specificity: Inhibits 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. Solubility: Soluble in anhydrous DMSO at 25mg/ml. Very poorly soluble in water. Applications: Suitable for use in in vitro or cell-based assays. Other applications not tested. Recommended Dilutions: May be further diluted into aqueous buffers to yield desired concentrations , (<100uM) with final DMSO concentrations of ~0.1%. IC50 values for inhibitory activity against MEK1 are around 5-10uM. For experiments with cultured cells, pretreat with M2865-17A for one hour prior to stimulation., Optimal dilutions to be determined by the researcher. Storage and Stability: Lyophilized powder is stable for 6 months after receipt at -20°C. Reconstitute with DMSO. Stable for 3 months Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap.