|2-((2-甲氧基-4-(4-甲基哌嗪-1-基)苯基)氨基)-5,11-二甲基-5,11-二氢-6H-苯并[e]嘧啶并[5,4-b][1,4]二氮杂卓-6-酮|CsnPharm

CAS No.: 1234479-76-5

ERK5-IN-1 Catalog No. CSN17601

Synonyms: XMD8-85

ERK5-IN-1 exhibits potent inhibition of ERK5 with cellular EC50 values of 0.19 μM and enzymatic IC50 values of 0.087 μM and of LRRK2[G2019S] with enzymatic IC50 values of 0.026μM.

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400-920-2911

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实验方案

技术信息

生物活性

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].
参考文献

[1] Deng X, Elkins JM, et al. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e] pyrimido-[5,4-b] diazepine-6(11H)-ones. Eur J Med Chem. 2013;70:758-767.
[2] Deng X, Elkins JM, Zhang J, Yang Q, Erazo T, Gomez N, Choi HG, Wang J, Dzamko N, Lee JD, Sim T, Kim N, Alessi DR, Lizcano JM, Knapp S, Gray NS. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur J Med Chem. 2013;70:758-67.
[3] Elkins JM, Wang J, Deng X, Pattison MJ, Arthur JS, Erazo T, Gomez N, Lizcano JM, Gray NS, Knapp S. X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor. J Med Chem. 2013 Jun 13;56(11):4413-21.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1761 mL
- 10.8804 mL
- 21.7607 mL
- 5 mM
- 0.4352 mL
- 2.1761 mL
- 4.3521 mL
- 10 mM
- 0.2176 mL
- 1.0880 mL
- 2.1761 mL

技术信息

CAS号

1234479-76-5

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H29N7O2

运输

蓝冰

分子量

459.54

别名

XMD8-85

溶解度

DMSO	100.0 mg/mL (217.6 mM)

动物实验配方

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