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513000

PD 98,059

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

Synonyme(s) :

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

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A propos de cet article

Formule empirique (notation de Hill) :
C16H13NO3
Numéro CAS:
167869-21-8
Poids moléculaire :
267.28
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD00671789
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Service technique
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Nom du produit

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

100

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)
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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

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Classe de stockage

11 - Combustible Solids

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