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XMD17-109 {[allProObj[0].p_purity_real_show]}

货号:A370232 同义名: ERK5-IN-1 Ambeed 开学季,买赠积分,赢豪礼

XMD17-109 is a specific ERK-5 inhibitor with an EC50 4.2 μM in HEK293 cells.

XMD17-109 化学结构 CAS号:1435488-37-1
XMD17-109 化学结构
CAS号:1435488-37-1
XMD17-109 3D分子结构
CAS号:1435488-37-1
XMD17-109 化学结构 CAS号:1435488-37-1
XMD17-109 3D分子结构 CAS号:1435488-37-1
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XMD17-109 纯度/质量文件 产品仅供科研

货号:A370232 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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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

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Pluripotin ++

ERK1, Kd: 98 nM

RasGAP {[allProObj[0].p_purity_real_show]}
FR 180204 +

ERK1, Ki: 0.31 μM

++

ERK2, Ki: 0.14 μM

{[allProObj[0].p_purity_real_show]}
Ravoxertinib +++

ERK1, IC50: 1.1 nM

++++

ERK2, IC50: 0.3 nM

{[allProObj[0].p_purity_real_show]}
SCH772984 +++

ERK1, IC50: 4 nM

++++

ERK2, IC50: 1 nM

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Temuterkib +++

ERK1, IC50: 5 nM

+++

ERK2, IC50: 5 nM

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VX-11e +++

ERK2, Ki: <2 nM

{[allProObj[0].p_purity_real_show]}
Ulixertinib ++++

ERK2, IC50: <0.3 nM

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XMD17-109 ++

ERK5, IC50: 162 nM

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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。

XMD17-109 生物活性

靶点
  • ERK5

    ERK5, IC50:162 nM

描述 MD17-109 inhibits ERK5 biochemically with an IC50 of 0.162 ± 0.006 μM and interrupts the epidermal growth factor-induced autophosphorylation of ERK5 in cells with an EC50 of 0.09 ± 0.03 μM. It also counteracts LRRK2[G2019S] with an IC50 of 339 nM[1]. XMD17-109 showcases potent nanomolar activity in cells, as demonstrated by a significant dose-responsive decrease in phosphorylated ERK5 mobility shift bands from sorbitol-stimulated cells. XMD17-109 fully inhibits ERK5-mediated AP1 transcriptional activity at 30 μM, with an EC50 value of 4.2 μM[2].
体外研究

MD17-109 inhibits ERK5 biochemically with an IC50 of 0.162 ± 0.006 μM and interrupts the epidermal growth factor-induced autophosphorylation of ERK5 in cells with an EC50 of 0.09 ± 0.03 μM. It also counteracts LRRK2[G2019S] with an IC50 of 339 nM[1].

XMD17-109 showcases potent nanomolar activity in cells, as demonstrated by a significant dose-responsive decrease in phosphorylated ERK5 mobility shift bands from sorbitol-stimulated cells. XMD17-109 fully inhibits ERK5-mediated AP1 transcriptional activity at 30 μM, with an EC50 value of 4.2 μM[2].

XMD17-109 参考文献

[1]Deng X, 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;70:758-67.

[2]Elkins, Jonathan M., et al. X-ray Crystal Structure of ERK5 (MAPK7) in Complex with a Specific Inhibitor. Journal of Medicinal Chemistry (2013), 56(11), 4413-4421.

XMD17-109 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.57mL

0.31mL

0.16mL

7.83mL

1.57mL

0.78mL

15.65mL

3.13mL

1.57mL

XMD17-109 技术信息

CAS号1435488-37-1
分子式C36H46N8O3
分子量 638.802
别名 ERK5-IN-1
运输蓝冰
存储条件

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(164.37 mM),配合低频超声,并水浴加热至45℃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

动物实验配方
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