513000

PD 98,059

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

• Synonyma: PD 98059, 2ʹ-Amino-3ʹ-methoxyflavone, MEK Inhibitor V
• Empirický vzorec (Hillův zápis): C₁₆H₁₃NO₃
• Číslo CAS: 167869-21-8
• Molekulová hmotnost: 267.28
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD00671789
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Vlastnosti

• Název produktu: 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

Popis

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 p140^trk 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)

Bezpečnostní informace

• Skladovací třída: 11 - Combustible Solids