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ERK5-IN-1 {[allProObj[0].p_purity_real_show]}

货号:A812686 同义名: 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.

ERK5-IN-1 化学结构 CAS号:1234479-76-5
ERK5-IN-1 化学结构
CAS号:1234479-76-5
ERK5-IN-1 3D分子结构
CAS号:1234479-76-5
ERK5-IN-1 化学结构 CAS号:1234479-76-5
ERK5-IN-1 3D分子结构 CAS号:1234479-76-5
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ERK5-IN-1 纯度/质量文件 产品仅供科研

货号:A812686 标准纯度: {[allProObj[0].p_purity_real_show]}
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全球学术期刊中引用的产品

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产品名称 ERK ERK1 ERK2 ERK5 其他靶点 纯度
DEL-22379 +

ERK, IC50: 0.5 μM

+

ERK, IC50: 0.5 μM

98%
Pluripotin ++

ERK1, Kd: 98 nM

RasGAP 98+%
FR 180204 +

ERK1, Ki: 0.31 μM

++

ERK2, Ki: 0.14 μM

98%
Ravoxertinib +++

ERK1, IC50: 1.1 nM

++++

ERK2, IC50: 0.3 nM

99%+
SCH772984 +++

ERK1, IC50: 4 nM

++++

ERK2, IC50: 1 nM

99%+
Temuterkib +++

ERK1, IC50: 5 nM

+++

ERK2, IC50: 5 nM

99%+
VX-11e +++

ERK2, Ki: <2 nM

99%+
Ulixertinib ++++

ERK2, IC50: <0.3 nM

99%+
XMD17-109 ++

ERK5, IC50: 162 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

ERK5-IN-1 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].

ERK5-IN-1 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.

ERK5-IN-1 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.88mL

2.18mL

1.09mL

21.76mL

4.35mL

2.18mL

ERK5-IN-1 技术信息

CAS号1234479-76-5
分子式C25H29N7O2
分子量 459.54
SMILES Code O=C1C2=C(C=CC=C2)N(C)C3=NC(NC4=C(OC)C=C(N5CCN(C)CC5)C=C4)=NC=C3N1C
MDL No. MFCD18642659
别名 XMD8-85
运输蓝冰
InChI Key DDTPGANIPBKTNU-UHFFFAOYSA-N
Pubchem ID 46844147
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, sealed in dry, 2-8°C

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
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