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生物化工
抑制劑
絲裂原活化蛋白激酶(MAPK)
MEK 抑制劑
2-(2-氨基-3-甲氧基苯基)-4H-1-苯并吡喃-4-酮
化合物 PD 98059
化合物 PD 98059|T2623
價格
¥
266
¥
378
¥
598
包裝
1mg
2mg
5mg
最小起訂量
1mg
發(fā)貨地
上海
更新日期
2024-12-02
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產品詳情
中文名稱:
化合物 PD 98059
英文名稱:
PD98059
CAS:
167869-21-8
品牌:
TargetMol
產地:
美國
保存條件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
純度規(guī)格:
99.66%
產品類別:
抑制劑
貨號:
T2623
2024-12-02
化合物 PD 98059
PD98059
1mg/266RMB;2mg/378RMB;5mg/598RMB
266
TargetMol
美國
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
99.66%
抑制劑
Product Introduction
Bioactivity
名稱
PD98059
描述
PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2/50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.
細胞實驗
The MCF10A-Neo and MCF10A-NeoT lines were derived by transfection of the MCF10A cell line with the pHo6 plasmid and the pHo6 plasmid containing an Ha-ras oncogene derived from the human T24 bladder carcinoma cell line, and subsequent selection for resistance to G418. The transfected lines represent pooled survivors, as opposed to clonal lines. With the exception of the EGF content being increased from 10 to 20 ng/ml, the cells were cultured in supplemented Dulbecco's modified Eagle's medium/Ham's F-12 medium in a humidified atmosphere of 95% air/5% CO2 at 37°C. Subconfluent cultures were treated with varying concentrations of chemicals dissolved in DMSO (absolute volume of solvent < 0.1% of medium volume). Subconfluent cultures are treated with PD98059 (0-100 μM). Viability of cells after treatment was assessed by ability to exclude trypan blue. Cultures earmarked for RNA isolation were washed twice with phosphate-buffered saline (2.7 mM KCl, 1.5 mM KH2PO4, 137mM NaCl, 8 mM Na2HPO4, pH 7.2) at harvesting and stored at 280°C [2].
激酶實驗
c-Raf and MEK kinase were measured by their ability to activate MAPKK1 (or MAPKK2) in a 30-min coupled assay containing MAPKK1 (or MAPKK2) and its substrate p42 MAP kinase. One unit of c-Raf or MEK kinase activity was that amount which increased the activity of p42Graphic by 1 unit/min. MAPKK was assayed directly in the cell lysate by the activation of bacterially expressed p42Graphic. One unit of MAPKK was that amount which increased the activity of p42Graphic by 1 unit/min. The assays of c-Raf and MAPKK are quantitative and extremely sensitive and are detailed elsewhere. p42Graphic was assayed by its ability to phosphorylate myelin basic protein and MAPKAP kinase 1 α/β by the phosphorylation of a peptide related to the C terminus of ribosomal protein S6 [Gly-245, Gly-246]S6-(218-249). One unit of p42Graphic or MAPKAP kinase-1α/β was that amount which catalyzed the phosphorylation of 1 nmol of substrate peptide in 1 min. Protein kinase activities in immunoprecipitates were measured by adding the other assay components to the tubes containing the immunoprecipitated enzyme [1].
動物實驗
Mice were randomized into 4 groups (n= 40 animals/group): (i) CAR + vehicle group. Mice were subjected to carrageenan-induced pleurisy and received the vehicle for PD98059 (10% dimethylsulfoxide (DMSO) (v/v) i.p. bolus 1 h after carrageen administration(N=10); (ii) PD98059 group. Same as the CAR + vehicle group but were administered PD98059 (10 mg/kg, i.p. bolus) 1 h after carrageenan administration (N=10); (iii) Sham+saline group. Sham-treated group in which identical surgical procedures to the CAR group were performed, except that the saline was administered instead of carrageenan (n=10); (iv) Sham+ PD98059 group. Identical to Sham+saline group except for the administration of PD98059 (10 mg/kg i.p. bolus) 1h after carrageenan administration of saline (N=10). The doses of PD98059 (10 mg/kg) used here were based on previous in vivo studies that demonstrated regulation of the inflammation process [4].
體外活性
方法
:人乳腺癌細胞 MCF-7 和 MDA-MB-231 用 PD98059 (1-50 μM) 處理 12-72 h,使用 MTT 方法檢測細胞活力。
結果
:PD98059 劑量依賴性和時間依賴性抑制乳腺癌腫瘤細胞增強。[1]
方法
:多藥耐藥性腫瘤細胞 SMMC7721/ADM 和 BEL7402/ADM 用 PD98059 (2.5-20 μM) 處理 1 h,使用 Western Blot 方法檢測靶點蛋白表達水平。
結果
:PD98059 用劑量依賴性方式下調細胞中的 pERK1/2 表達率。[2]
體內活性
方法
:為檢測對非感染性休克的影響,將 PD98059 (10 mg/kg) 腹腔注射給酵母多糖誘導非感染性休克的 CD 小鼠。
結果
:用 PD98059 治療顯著降低了酵母多糖引起的全身毒性、體重減輕和死亡率。[3]
方法
:為研究對實驗性自身免疫性腦炎 (EAE) 的作用,將 PD98059 (5 mg/kg) 腹腔注射給 EAE 的 SJL/J 小鼠模型,每天一次,持續(xù)兩周。
結果
:PD98059 可以糾正 EAE 小鼠的免疫功能障礙,這與多種信號通路的調節(jié)同時發(fā)生。[4]
存儲條件
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 0.67 mg/mL (2.51 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
Ethanol : 1.3 mg/mL (5 mM)
DMSO : 13.75 mg/mL (51.44 mM), Sonication is recommended.
關鍵字
AhR | Extracellular signal regulated kinases | PD98059 | MAP2K | ERK | MAPKK | Autophagy | Aryl Hydrocarbon Receptor | inhibit | Mitogen-activated protein kinase kinase | Inhibitor | PD-98059 | MEK
相關產品
Guanidine hydrochloride | Naringin | Valproic Acid | Taurine | Gefitinib | Aceglutamide | Hydroxychloroquine | Curcumin | Stavudine | Salicylic acid | Paeonol | Sodium 4-phenylbutyrate
相關庫
抑制劑庫 | 經典已知活性庫 | 已知活性化合物庫 | 自噬庫 | 激酶抑制劑庫 | 抗衰老化合物庫 | HIF-1化合物庫 | 干細胞分化化合物庫 | 酪氨酸激酶分子庫 | 疼痛相關化合物庫
關鍵字:
PD 98059|TargetMol
公司簡介
上海陶術生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起,為北美、歐洲和亞洲從事藥物研發(fā)和生物學研究的科學家提供優(yōu)質的產品和專業(yè)的服務。公司下設篩選事業(yè)部,化學事業(yè)部,生物事業(yè)部和新材料部。 從虛擬篩選到實體化合物分子供應;從商業(yè)化產品銷售到個性化定制合成;從對明確靶點的分子篩選到對明確分子的多靶點篩選,從高通量篩選到化學結構優(yōu)化,我們都可以滿足您的科研用品及技術服務的需求。 經過在中國市場五年的精心耕耘,我們已成為篩選化合物領域優(yōu)秀的供應商,為超過五百家學校和各類企業(yè)提供了品質卓越的小分子化合物和藥物篩
成立日期
2013-04-18
(12年)
注冊資本
566.2651萬人民幣
員工人數(shù)
100-500人
年營業(yè)額
¥ 1億以上
主營行業(yè)
化學試劑,生物活性小分子
經營模式
貿易,試劑,定制,服務
TargetMol中國(陶術生物)
VIP
12年
公司成立:
12年
注冊資本:
566.2651萬人民幣
企業(yè)類型:
有限責任公司(自然人投資或控股)
主營產品:
小分子抑制劑,藥物篩選化合物庫,天然產物,活性分子化合物等
公司地址:
上海市閘北區(qū)江場三路28號4樓
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