Brief Description

XMD17-109 is a novel, specific ERK-5 inhibitor with an EC50 4.2 uM in HEK293 cells. IC50 Value: 4.2±0.69 uM(EC50, inhibits ERK5-mediated AP1 transcriptional activity in HEK 293 cells) Target: ERK5 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.

Solubility

DMSO

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Density

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Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

Light yellow to yellow solid