513000
PD 98,059
≥98% (HPLC), solid, MEK inhibitor, Calbiochem®
Synonym(s):
PD 98059, 2ʹ-Amino-3ʹ-methoxyflavone, MEK Inhibitor V
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About This Item
Empirical Formula (Hill Notation):
C16H13NO3
CAS Number:
Molecular Weight:
267.28
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Product Name
PD 98059, PD 98059, CAS 167869-21-8, is a cell-permeable, selective & reversible inhibitor of MAP Kinase Kinase (MEK). Inhibits MAP Kinase activation and subsequent phosphorylation of MAP Kinase substrates.
Quality Segment
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
pale yellow
solubility
methanol: 0.7 mg/mL, DMSO: 20 mg/mL
shipped in
ambient
storage temp.
−20°C
SMILES string
Nc1c(cccc1c2[o]c3c([c](c2)=O)cccc3)OC
InChI
1S/C16H13NO3/c1-19-14-8-4-6-11(16(14)17)15-9-12(18)10-5-2-3-7-13(10)20-15/h2-9H,17H2,1H3
InChI key
QFWCYNPOPKQOKV-UHFFFAOYSA-N
General description
Selective, reversible, and cell-permeable inhibitor of MAP kinase kinase (MEK) that acts by inhibiting the activation of MAP kinase and subsequent phosphorylation of MAP kinase substrates. Pretreatment of PC-12 cells with PD 98059 completely blocks the 4-fold increase in MAP kinase activity produced by nerve growth factor (NGF; IC50 = 2 µM); however, it has no effect on NGF-dependent tyrosine phosphorylation of the p140trk receptor or its substrate Shc and does not block NGF-dependent activation of PI 3-kinase. Blocks LPS-induced activation of TNF-α gene expression. Inhibits cell growth and reverses the phenotype of ras-transformed BALB3T3 mouse fibroblasts and rat kidney cells. A 5 mg/ml solution of PD 98059 (Cat. No. 513001) in anhydrous DMSO is also available.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
MAP kinase kinase (MEK)
MAP kinase kinase (MEK)
Product does not compete with ATP.
Reversible: yes
Target IC50: 2 µM against NGF-induced increase in MAP kinase activity
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 4 months at -20°C.
Other Notes
Means, T.K., et al. 2000. J. Leukoc. Biol. 67, 885.
Kültz, D., et al. 1998. J. Biol. Chem. 273, 13645.
Dudley, D.T., et al. 1995. Proc. Natl. Acad. Sci. USA92, 7686.
Langlois, W.J., et al. 1995. J. Biol. Chem. 270, 25320.
Pang, L., et al. 1995. J. Biol. Chem.270, 13585.
Waters, S.B., et al. 1995. J. Biol. Chem.270, 20883.
Kültz, D., et al. 1998. J. Biol. Chem. 273, 13645.
Dudley, D.T., et al. 1995. Proc. Natl. Acad. Sci. USA92, 7686.
Langlois, W.J., et al. 1995. J. Biol. Chem. 270, 25320.
Pang, L., et al. 1995. J. Biol. Chem.270, 13585.
Waters, S.B., et al. 1995. J. Biol. Chem.270, 20883.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
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Storage Class
11 - Combustible Solids
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