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Merck
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Documentos Principais

513000

Sigma-Aldrich

PD 98059

≥98% (HPLC), solid, MEK inhibitor, Calbiochem®

Sinônimo(s):

PD 98059, 2ʹ-Amino-3ʹ-methoxyflavone, MEK Inhibitor V

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About This Item

Fórmula empírica (Notação de Hill):
C16H13NO3
Número CAS:
Peso molecular:
267.28
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77

Nome do produto

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.

Nível de qualidade

Ensaio

≥98% (HPLC)

Formulário

solid

fabricante/nome comercial

Calbiochem®

condição de armazenamento

OK to freeze
protect from light

cor

pale yellow

solubilidade

methanol: 0.7 mg/mL
DMSO: 20 mg/mL

Condições de expedição

ambient

temperatura de armazenamento

−20°C

cadeia de caracteres SMILES

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

chave InChI

QFWCYNPOPKQOKV-UHFFFAOYSA-N

Descrição geral

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.

Ações bioquímicas/fisiológicas

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

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 4 months at -20°C.

Outras notas

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.

Informações legais

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

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3


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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.
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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
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
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
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Journal of biomedical science, 10(6 Pt 2), 738-745 (2003-11-25)
The type-I plasminogen activator inhibitor (PAI-1), the primary inhibitor of both tissue-type and urokinase-type plasminogen activators (t-PA, u-PA), is the primary regulator of plasminogen activation and possibly of extracellular proteolysis. In anchorage-dependent cells, the PAI-1 gene is regulated by cell

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