ERK5-IN-1
产品说明书
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同义名 : | XMD8-85 |
| CAS号 : | 1234479-76-5 | |
| 货号 : | A812686 | |
| 分子式 : | C25H29N7O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 459.54 | |
| MDL号 : | MFCD18642659 | |
| 存储条件： |
Pure form Keep in dark place, sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | ERK5, encoded by MAPK7 gene, is a member of the MAP kinase family. ERK5 plays a role in various cellular processes such as proliferation, differentiation and cell survival. The upstream activator of ERK5 is the MAPK kinase MAP2K5. Upon activation, ERK5 translocates to the nucleus and phosphorylates various downstream targets. ERK5-IN-1 is an ERK5 selective inhibitor with IC50 of 162nM[2]. At the concentrations of 0.04, 0.2, 1 and 5μM, ERK5-IN-1 concentration-dependently inhibited ERK5 autophosphorylation stimulated by sorbitol in Hela cells. ERK5-IN-1 also inhibited ERK5-mediated AP1 transcriptional activity with an EC50 of 4.2μM, and constitutively active MEK5 co-transfected HEK293 cell system[3]. In mice, the oral bioavailability of ERK5-IN-1 was 90%[2]. | ||
| 作用机制 | ERK5-IN-1 target ERK5 in an ATP competitive manner[3]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.18mL 0.44mL 0.22mL |
10.88mL 2.18mL 1.09mL |
21.76mL 4.35mL 2.18mL |
| 参考文献 |
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