化合物 PD 98059|T2623

PD98059
167869-21-8

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上海更新日期：2024-09-14

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产品详情:

中文名称：: 化合物 PD 98059

英文名称：: PD98059

CAS号：: 167869-21-8

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.66%

产品类别：: 抑制剂

货号：: T2623

Product Introduction

Bioactivity

名称	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.
细胞实验	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].
激酶实验	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].
动物实验	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].
体外活性	方法：人乳腺癌细胞 MCF-7 和 MDA-MB-231 用 PD98059 (1-50 μM) 处理 12-72 h，使用 MTT 方法检测细胞活力。结果：PD98059 剂量依赖性和时间依赖性抑制乳腺癌肿瘤细胞增强。[1] 方法：多药耐药性肿瘤细胞 SMMC7721/ADM 和 BEL7402/ADM 用 PD98059 (2.5-20 μM) 处理 1 h，使用 Western Blot 方法检测靶点蛋白表达水平。结果：PD98059 用剂量依赖性方式下调细胞中的 pERK1/2 表达率。[2]
体内活性	方法：为检测对非感染性休克的影响，将 PD98059 (10 mg/kg) 腹腔注射给酵母多糖诱导非感染性休克的 CD 小鼠。结果：用 PD98059 治疗显著降低了酵母多糖引起的全身毒性、体重减轻和死亡率。[3] 方法：为研究对实验性自身免疫性脑炎 (EAE) 的作用，将 PD98059 (5 mg/kg) 腹腔注射给 EAE 的 SJL/J 小鼠模型，每天一次，持续两周。结果：PD98059 可以纠正 EAE 小鼠的免疫功能障碍，这与多种信号通路的调节同时发生。[4]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : 1.3 mg/mL (5 mM) DMSO : 13.75 mg/mL (51.44 mM), Sonication is recommended.
关键字	AhR \| Extracellular signal regulated kinases \| PD98059 \| MAP2K \| ERK \| MAPKK \| Autophagy \| Aryl Hydrocarbon Receptor \| inhibit \| Mitogen-activated protein kinase kinase \| Inhibitor \| PD-98059 \| MEK
相关产品	Oxyresveratrol \| Guanidine hydrochloride \| Naringin \| Taurine \| Gefitinib \| Xylitol \| Hydroxychloroquine \| Curcumin \| Stavudine \| Myricetin \| Paeonol \| Sodium 4-phenylbutyrate
相关库	抑制剂库 \| 经典已知活性库 \| 已知活性化合物库 \| 自噬库 \| 激酶抑制剂库 \| 抗衰老化合物库 \| HIF-1化合物库 \| 干细胞分化化合物库 \| 酪氨酸激酶分子库 \| 疼痛相关化合物库

PD 98059

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子