PD98059
产品说明书
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同义名 : | NSC 679828 |
| CAS号 : | 167869-21-8 | |
| 货号 : | A282482 | |
| 分子式 : | C16H13NO3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 267.28 | |
| MDL号 : | MFCD00671789 | |
| 存储条件： |
Pure form Sealed in dry, store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 35 mg/mL(130.95 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | MEKs, which are members of the MAPKK family, can activate both ERK1 and ERK2 by catalyzing the phosphorylation on T202/Y204. Also MEK itself can be phosphorylated and activated through Ras when the upstream signaling is activated by extracellular stimuli, including growth factors, hormones etc.. PD98059 is MEK1/2-specific inhibitor with IC50=~10uM (measured by phosphorylation level of MAPK-KA catalyzed by GST-MEK1) with no effect on ERK. Pre-incubation of PD98059 can inhibit PDGF-stimulated tyrosine phosphorylation of MAPK while preventing thymidine incorporation with an IC50 of 7 uM in 3T3 cells. PD98059 did not show significant inhibitory activity on Raf kinase, cAMP-dependent kinase, protein kinase C, v-Src, EGF receptor kinase, insulin receptor kinase, PDGFreceptor kinase, and PI3Ks, which shows the high selectivity of it [1]. PD98059 is the first generation small molecule inhibitors of MEK1/2. PD98059 does not interfere with Raf access to MEK1/2 for it did not affect serum-induced MEK1/2 phosphorylation [2]. | ||
| 作用机制 | PD 098059 does not complete for ATP binding or MAPK binding to MEK and most likely inhibits through an allosteric mechanism.[1] | ||
| 细胞研究 | |||||
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| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
| 7402 | 30 μM | Apoptosis Assay | 5 d | decreases cell proliferation | 24211253 |
| 7721 | 30 μM | Apoptosis Assay | 5 d | decreases cell proliferation | 24211253 |
| 786-O | 50 μM | Apoptosis Assay | 24 h | potentiates the pro-apoptotic effects of NC | 24508476 |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.74mL 0.75mL 0.37mL |
18.71mL 3.74mL 1.87mL |
37.41mL 7.48mL 3.74mL |
