目錄:愛必信（上海）生物科技有限公司>>生化試劑>>小分子化合物>> abs810010PD 98059
| 參考價 | 139 |
參考價：￥ 139
5mg
CAS:167869-21-8 純度:>98 % 分子量:267.28 分子式:C16H13NO3 供貨周期:現貨 規(guī)格:5mg;10mg;50mg 貨號:abs810010 應用領域:化工,生物產業(yè),農林牧漁,制藥/生物制藥,綜合 主要用途:是一種非ATP競爭性的MEK抑制劑
>| 5mg | 139元 | 999份可售 |
更新時間：2025-11-04 14:53:42瀏覽次數：1842評價
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| CAS | 167869-21-8 | 純度 | >98 % |
|---|---|---|---|
| 分子量 | 267.28 | 分子式 | C16H13NO3 |
| 供貨周期 | 現貨 | 規(guī)格 | 5mg;10mg;50mg |
| 貨號 | abs810010 | 應用領域 | 化工,生物產業(yè),農林牧漁,制藥/生物制藥,綜合 |
| 主要用途 | 是一種非ATP競爭性的MEK抑制劑 |
| 產品描述 | |
| 描述 | PD 98059是一種非ATP競爭性的MEK抑制劑，無細胞試驗中IC50為2 μM，特異性抑制MEK-1介導的MAPK激活；不直接抑制ERK1或ERK2。PD 98059不會抑制已經被c-Raf磷酸化的 MEK1。 |
| 純度 | >98 % |
| 儲存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | PD-98059,PD98059 |
| 外觀 | Lyophilized powder |
| 可溶性/溶解性 | DMSO：14 mg/mL warmed (52.37 mM) |
| 生物活性 | |
| 靶點 | MEK1 |
| In vitro(體外研究) | 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. PD98059 does not inhibit the MAPK homologues JNK and P38. PD98059 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. PD98059 inhibits PDGF-stimulated activation of MAPK and thymidine incorporation into 3T3 cells with IC50 of ~10 μM and ~7 μM, respectively. PD98059 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. PD98059 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. PD98059 completely blocks the nerve growth factor (NGF)-induced differentiation of PC12 cells without altering cell viability. PD98059 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. |
| In vivo(體內研究) | Treatment of mice 30 minutes before focal cerebral ischemia with PD98059 protects against damage, resulting in a decrease in infarct volume. Pretreated with PD98059 (10 mg/kg per i.v. injection) 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. Administration of PD98059 (10 mg/kg) in mice 1 hour after carrageenan causes a reduction in all the parameters of inflammation measured. |
| 參考文獻 | |
| 參考文獻 | [1] Dudley DT, et al. Proc Natl Acad Sci U S A, 1995, 92(17), 7686-7689. [2] Alessi DR, et al. J Biol Chem, 1995, 270(46), 27489-27494. [3] Pang L, et al. J Biol Chem, 1995, 270(23), 13585-13588. |
| 研究領域 | |
| 研究領域 | Signal TransductionProtein PhosphorylationSer / Thr KinasesMAPK Pathway Signal TransductionProtein PhosphorylationTyrosine KinasesOther Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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