PD98059

製品コードS1177 バッチS117709

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H13NO3
分子量 267.28 CAS No. 167869-21-8
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 28 mg/mL (104.75 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 1.000mg/ml (3.74mM) Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist.
in vitro

PD98059 inhibits either basal MEK1 or a partially activated MEK produced by mutation of serine at residues 218 and 222 to glutamate (MEK-2E) with IC50 of 2 μM. This compound does not inhibit the MAPK homologues JNK and P38. It is highly selective against MEK, as it does not inhibit a number of other kinase activities including Raf kinase, cAMP-dependent kinase, protein kinase C, v-Src, epidermal growth factor (EGF) receptor kinase, insulin receptor kinase, PDGF receptor kinase, and phosphatidylinositol 3-kinase. This inhibitor inhibits PDGF-stimulated activation of MAPK and thymidine incorporation into 3T3 cells with IC50 of ~10 μM and ~7 μM, respectively. [1] It potently prevents the activation of MEK1 by Raf or MEK kinase with IC50 of 4 μM, and weakly inhibits the activation of MEK2 by Raf with IC50 of 50 μM. This chemical does not inhibit the activation of MEK homologues MKK4 and RK kinase that participate in stress and interleukin-1-stimulated kinase cascades in KB and PC12 cells, and the activation of p70 S6 kinase by insulin or epidermal growth factor in Swiss 3T3 cells. [2] It completely blocks the nerve growth factor (NGF)-induced differentiation of PC12 cells without altering cell viability. [3] This compound inhibits the proliferation of RAW264.7 cells in the culture containing RANKL in a dose-dependent manner, resulting in an apparent decrease of TRAP-positive cells. [4]
in vivo

Treatment of mice 30 minutes before focal cerebral ischemia with PD98059 protects against damage, resulting in a decrease in infarct volume. [5] Pretreated with this compound 30 minutes before and then together with hourly cerulein injections for 3 hours significantly ameliorates cerulein-induced acute pancreatitis ipancreatitis on the basis of pancreatic wet weight and histology. [6] Administration of this chemical (10 mg/kg) in mice 1 hour after carrageenan causes a reduction in all the parameters of inflammation measured. [7]
特徴 Does not inhibit c-Raf phosphorylated MEK1.

プロトコル(参考用のみ)

キナーゼアッセイ In vitro MEK-inhibitory activity
Incorporation of 32P into myelin basic protein (MBP) is assayed in the presence of glutathione S-transferase (GST) fusion proteins containing the 44-kDa MAPK (GST-MAPK) or the 45-kDa MEK (GST-MEK1). Assays are conducted in 50 μL of 50 mM Tris, pH 7.4/10 mM MgCl2/2 mM EGTA/10 μM [γ-32P]ATP containing 10 μg of GST-MEK1, 0.5 μg of GST-MAPK, and 40 μg of MBP. After incubation at 30°C for 15 minutes, reactions are stopped by addition of Laemmli SDS sample buffer. Phosphorylated MBP is resolved by SDS/10% PAGE.
細胞アッセイ 細胞株 K-Balb, KNRK, v-raf-3Y1, SRA/3Y1, EGFR/3T3, and K562
濃度 Dissolved in DMSO, final concentrations ~100 μM
反応時間 3 dyas, or 7-10 days
実験の流れ

For monolayer growth, cells are plated into multi-well plates at 10,000-20,000/mL. Forty-eight hours later, various concentrations of PD98059 are added to the cell growth medium and incubation is continued for an additional 3 days. Cells are then removed from the wells by incubation with trypsin and enumerated with a Coulter Counter. For growth in soft agar, cells are seeded into 35-mm dishes at 5,000-10,000 cells per dish with growth medium containing 0.3% agar and desired concentrations of this compound. After 7-10 days of growth, visible colonies are manually enumerated with the aid of a dissecting microscope.
動物実験 動物モデル Male Sprague–Dawley rats with acute pancreatitis
投薬量 10 mg/kg
投与方法 Injection i.v.

参考

  • https://pubmed.ncbi.nlm.nih.gov/7644477/
  • https://pubmed.ncbi.nlm.nih.gov/7499206/
  • https://pubmed.ncbi.nlm.nih.gov/7775407/
  • https://pubmed.ncbi.nlm.nih.gov/12237315/
  • https://pubmed.ncbi.nlm.nih.gov/10536014/
  • https://pubmed.ncbi.nlm.nih.gov/12370536/
  • https://pubmed.ncbi.nlm.nih.gov/20074457/
  • https://pubmed.ncbi.nlm.nih.gov/11254111/
  • https://pubmed.ncbi.nlm.nih.gov/17161815/
  • https://pubmed.ncbi.nlm.nih.gov/14506750/
  • https://pubmed.ncbi.nlm.nih.gov/17409429/
  • https://pubmed.ncbi.nlm.nih.gov/9495809/

カスタマーフィードバック

Data from [Microbes Infect, 2013, 15, 105-14]

Data from [J Natl Cancer Inst, 2012, 104(21), 1673-9]

Data from [J Natl Cancer Inst, 2012, 104(21), 1673-9]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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