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(Top):

Western blot analysis of extracts from SK-N-MC cells untreated or treated with Human Basic Fibroblast Growth Factor (hFGF basic/FGF2) #8910 (100 ng/ml, 30 min; +) either with or without PD98059 pretreatment (1 hr) at the indicated concentrations, using Phospho-p44/42 MAPK (Erk1/2) (Thr202/Tyr204) Antibody #9101.

(Middle):

Western blot analysis of extracts from COS cells transfected with pCMV-MKK3 (22 hrs), untreated or treated with Anisomycin #2222 (20 ug/ml; 30min; +) either with or without PD98059 pretreatment (1 hr) at the indicated concentrations, using Phospho-MKK3 (Ser189)/MKK6 (Ser207) Antibody #9231.

(Bottom):

Western blot analysis of extracts from 293 cells untreated or treated with sodium chloride (NaCl) (0.7 Ml; 30min; +) either with or without PD98059 pretreatment (1 hr) at the indicated concentrations, using Phospho-SEK1/MKK4 (Thr261) Antibody #9151.

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Product Usage Information

PD98059 is supplied as a lyophilized powder. For a 20mM stock, reconstitute 1.5mg in 280 μl anhydrous DMSO (5 mg in 933.3 μl anhydrous DMSO). For 50mM stock, reconstitute 1.5 mg in 112 μl anhydrous DMSO (5 mg in 373.3 μl). Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 5 - 50 μM for one hour prior to treating with a stimulator.


Storage: Store lyophilized or in solution at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight:

267.28 g/mol


Purity:

>99%


Molecular Formula:

C16H13NO3


Bioactivity:

Solubility: Soluble in anhydrous DMSO at 25mg/ml. Very poorly soluble in water.


MEK1 and MEK2, also called MAPK or Erk kinases, are dual-specificity protein kinases that function in a mitogen activated protein kinase cascade controlling cell growth and differentiation (1-3). Activation of MEK1 and MEK2 occurs through phosphorylation of two serine residues at positions 217 and 221, located in the activation loop of subdomain VIII, by Raf-like molecules. MEK1/2 is activated by a wide variety of growth factors and cytokines and also by membrane depolarization and calcium influx (1-4). Constitutively active forms of MEK1/2 are sufficient for the transformation of NIH/3T3 cells or the differentiation of PC-12 cells (4). MEK activates p44 and p42 MAP kinase by phosphorylating both threonine and tyrosine residues at sites located within the activation loop of kinase subdomain VIII.

PD98059 has been shown to act in vitro 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).

PD98059 inhibits activation of MEK1 and MEK2 with IC50 values of 4 µM and 50 µM, respectively (1-3). Research has demonstrated 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 100 µM, PD98059 does not inhibit activation of MKK3 or SEK (MKK4). We have also found no inhibition of MKK6 or related family members.


1.  Crews, C.M. et al. (1992) Science 258, 478-480.

2.  Alessi, D.R. et al. (1994) EMBO J. 13, 1610-1619.

3.  Rosen, L.B. et al. (1994) Neuron 12, 1207-1221.

4.  Cowley, S. et al. (1994) Cell 77, 841-852.

5.  Crews, C.M. et al. (1992) Science 258, 478-480.

6.  Alessi, D.R. et al. (1994) EMBO J. 13, 1610-1619.

7.  Rosen, L.B. et al. (1994) Neuron 12, 1207-1221.

8.  Cowley, S. et al. (1994) Cell 77, 841-852.



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