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513000

Sigma-Aldrich

PD 98059

≥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
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

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 Level

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

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 (noncompetitive with respect to ATP). Pretreatment of PC-12 cells with PD 98059 completely blocks the 4-fold increase of MAP kinase activity produced by nerve growth factor (NGF; IC50 = 2 µM); however, it has no effect on NGF-dependent tyrosine phosphorylation of the pp140trk receptor or its substrate Shc and does not block NGF-dependent activation of PI 3-kinase. Inhibits cell growth and reverses the phenotype of ras-transformed BALB 3T3 mouse fibroblasts and rat kidney cells.
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)
Product does not compete with ATP.
Reversible: yes
Target IC50: 2 µM against NGF-induced increase in MAP kinase activity

Warning

Toxicity: Standard Handling (A)

Reconstitution

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 3


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Wenjuan Sun et al.
Frontiers in pharmacology, 13, 807452-807452 (2022-05-03)
Inflammation and apoptosis are the major contributors to the mechanisms of acute kidney injury (AKI) due to renal ischemia-reperfusion injury (IRI). Maslinic acid (MA), a pentacyclic triterpene acid mostly found in dietary plants, the current study was to demonstrate the
Geetha Yadav et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 23(31), 10021-10031 (2003-11-07)
Chick pineal cells in culture display a circadian rhythm of melatonin release. Light pulses can entrain (phase shift) the rhythm. One candidate for the photoentrainment pathway uses a mitogen-activated protein kinase (MAPK), also known as extracellular signal-regulated kinase (ERK). We
Sara Manzano et al.
Cell death & disease, 12(4), 348-348 (2021-04-08)
Glioblastoma (GBM) is the most aggressive tumor from the central nervous system (CNS). The current lack of efficient therapies makes essential to find new treatment strategies. C3G, a guanine nucleotide exchange factor for some Ras proteins, plays a dual role
Christina L Sherry et al.
Journal of immunology (Baltimore, Md. : 1950), 178(2), 663-670 (2007-01-05)
Dysregulated inflammation is a complication of type 2 diabetes (T2D). In this study, we show that augmented LPS-induced TNF-alpha production by resident peritoneal macrophages (PerMphi) in type 2 diabetic (db/db) mice is dependent on elevated glucose and requires p38 MAPK.
C E Poteet-Smith et al.
The Journal of biological chemistry, 274(32), 22135-22138 (1999-07-31)
p90 ribosomal S6 kinases (RSKs), containing two distinct kinase catalytic domains, are phosphorylated and activated by extracellular signal-regulated kinase (ERK). The amino-terminal kinase domain (NTD) of RSK phosphorylates exogenous substrates, whereas the carboxyl-terminal kinase domain (CTD) autophosphorylates Ser-386. A conserved

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