PD-98059

  • 来源:上海康成生物工程有限公司
  • 时间: 2008/1/30
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    PD-98059

    2’-Amino-3’-methoxyflavone

     

    Catalog No: KC-4P001

    Size: 5 mg

     

     

    Physical Appearance:  Pale yellow solid

     

    Molecular Formula:  C16H13NO3

     

    Molecular Weight:  267.3

     

    Purity:  >99% (TLC)

     

    Solubility:  DMSO (20 mg/ml) and methanol (0.7 mg/ml)

     

    Storage:  FREEZER (-20℃). Protect from light. Following reconstitution, aliquot and freeze (-20℃). This product is stable for 2 years as supplied. Stock solutions are stable for up to 3 months at -20℃.

    SK-N-MC cells were pretreated with different amounts of PD98059 (MEK1 Inhibitor) for 1 hour, then treated with FGF for 30 minutes. Cell extracts were blotted with Phospho-p44/p42 MAP Kinase (Thr202/Tyr204) Antibody (top). COS cells were transfected with pCMV-MKK3 for 22 hours, pretreated with different amounts of PD98059 for 1 hour, then treated with ani-somycin for 30 minutes. Cell extracts were blotted with Phospho-MKK3/MKK6 (Ser189/207) Antibody (middle). 293 cells were pretreated with different amounts of PD98059 for 1 hour, then treated with sodium chloride for 30 minutes. Cell extracts were blotted with Phospho-SEK1/MKK4 (Thr261) Antibody (bottom).

    Background:  PD98059 (MEK Inhibitor) has been shown to act in vivo as a highly selective inhibitor of MEK activation and the MAP kinase cascade. PD98059 binds to the inactive forms of MEK and prevents activation by upstream activators such as c-Raf.

     

    Description:  PD98059 (MEK Inhibitor) is soluble in DMSO at 10–100 mM. For use with in vitro or cell-based assays, it may be diluted into aqueous buffers to yield desired concentrations (<100 µM) with final DMSO concentrations of ~0.1%. IC50 values for inhibitory activity against MEK1 are around 5–10 µM. For experiments with cultured cells, we recommends pretreating with this inhibitor for one hour prior to stimulation.

     

    Specificity:  PD98059 (MEK1 Inhibitor) inhibits activation of MEK1 and MEK2 with IC50 values of 4 µM and 50 µM, respectively. Testing by us 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. As shown in the Western blot, at concentrations up to 100 µM PD98059 does not inhibit activation of MKK3 or SEK (MKK4) as determined by measuring phospho-rylation at its activation site. We have also found no inhibition of MKK6 or related family members.

     

    Directions for Use:  Supplied as a lyophilized yellow powder. For 20 mM stock, reconstitute 5 mg in 933 µl DMSO. For 50 mM stock, reconstitute 5 mg in 373 µl DMSO. Store in aliquots at –20°C. See enclosed MSDS or refer to our website for further information.

     

    References:

    1.      D.R.Alessi et al. J.Biol.Chem. 1995 270 27489

    2.      L.Pang et al. J.Biol.Chem. 1995 270 13585

     

    The pharmacological and toxicological properties of this product have not been fully investigated.  Exercise caution in use and handling. This product must not be used in humans

     

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