Biological Activity of XMD17-109

Description:
IC50 Value: 4.2±0.69 uM(EC50, inhibits ERK5-mediated AP1 transcriptional activity in HEK 293 cells) [1]
XMD17-109 is a novel, specific ERK-5 inhibitor with an EC50 4.2uM in HEK293 cells.
In vitro: The pAP1-luciferase reporter and pRL-CMV-Renilla plasmids were co-transfected with plasmids encoding for ERK5 and constitutively active MEK5 (MEK5DD) in HEK293 cells. Cells were treated with the indicated amounts of compound 26 (XMD17-109) for 24 h, and lysates were subjected to the dual-luciferase assay. Compound 26 completely inhibited the ERK5-mediated AP1 transcriptional activity at 30 μM and had an EC50 of 4.2 ± 0.7 μM. By contrast 24 had an EC50 of >30 μM[1].
in vivo: N/A
Clinical trial: N/A
 

References on XMD17-109

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