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XMD17-109

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Chemical Structure| 1435488-37-1 同义名 : ERK5-IN-1
CAS号 : 1435488-37-1
货号 : A370232
分子式 : C36H46N8O3
纯度 : 99%+
分子量 : 638.802
MDL号 : MFCD26142929
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：
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].
实验方案
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
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.