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 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Aiptasia larvae
1 μM
1 h
Inhibition of ERK5 activity reduced the retention of symbionts in host cells and increased the expulsion of symbionts.
Nat Microbiol. 2021 Jun;6(6):769-782.
J774.A1 cells
1 µM
18 h
Inhibition of ERK5 activity significantly increased vomocytosis rates in J774.A1 cells.
Sci Adv. 2017 Aug 16;3(8):e1700898.
Human PBMC-derived macrophages
1 µM
18 h
Inhibition of ERK5 activity significantly increased vomocytosis rates in human PBMC-derived macrophages.
Sci Adv. 2017 Aug 16;3(8):e1700898.
HMVEC-lung cells
1 μM
6 h
Inhibited the secretion of IL-6 and IL-8, indicating the role of ERK5 in inflammatory responses
Sci Signal. 2015 Aug 25;8(391):ra86.
HUVECs
1 μM
6 h
Inhibited the secretion of IL-6 and IL-8, indicating the role of ERK5 in inflammatory responses
Sci Signal. 2015 Aug 25;8(391):ra86.
PBMCs
1 μM
6 h
Inhibited the secretion of IL-6 and IL-8, indicating the role of ERK5 in inflammatory responses
Sci Signal. 2015 Aug 25;8(391):ra86.
monocytes
1 μM
6 h
Inhibited the secretion of IL-6 and IL-8, indicating the role of ERK5 in inflammatory responses
Sci Signal. 2015 Aug 25;8(391):ra86.
XMD17-109 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
LPS-induced endotoxemia model
Intraperitoneal injection
50 mg/kg
Single dose, monitored for up to 72 hours
Inhibition of ERK5 activity significantly improved survival rates in mice
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