513000

PD 98059

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

• 別名: PD 98059, 2ʹ-Amino-3ʹ-methoxyflavone, MEK Inhibitor V
• 実験式（ヒル表記法）: C₁₆H₁₃NO₃
• CAS番号: 167869-21-8
• 分子量: 267.28
• MDL番号: MFCD00671789
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 製品名: 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.
• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: pale yellow
• 溶解性: methanol: 0.7 mg/mL; DMSO: 20 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C
• SMILES記法: 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

詳細

詳細

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 pp140^trk 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 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.

生物化学的／生理学的作用

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

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3